- Spectroscopy, electrochemistry, and structure of 3d-transition metal complexes of thiosemicarbazones with quinoline core: Evaluation of antimicrobial property
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A series of Co(II), Ni(II), Cu(II), and Zn(II) complexes of quinoline-thiosemicarbazones was prepared. The Schiff base ligands that provide N, O, and S donor atoms for ligation are synthesized by the condensation of 2-hydroxy-3-formylquinoline with substituted thiosemicarbazides in ethanol. The ligands and complexes are characterized by elemental analysis, infrared, 1H NMR, UV-Vis, fast atom bombardment (FAB) mass spectroscopy, and electron spin resonance (ESR) spectral studies followed by magnetic susceptibility and conductivity measurements. The ligand-to-metal ratio is found to be 1:1 and 2:2 for the complexes of L1H2 and LcH2, respectively. All the complexes are found to have octahedral geometry except [CuL1H(H2O)Cl], which exhibits a square pyramidal structure. All the complexes are nonelectrolytic in nature and the electrochemical behavior of complexes is dealt with briefly. Further ligands and complexes were evaluated for their antimicrobial activity against bacteria Escherichia coli and Pseudomonas aeruginosa and fungi Aspergillus niger and Cladosporidium. Taylor & Francis Group, LLC.
- Kulkarni, Naveen V.,Hegde, Ganesh S.,Kurdekar, Gurunath S.,Budagumpi, Srinivasa,Sathisha,Revankar, Vidyanand K.
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- A highly selective chemosensor for Al3+ based on 2-oxo-quinoline-3-carbaldehyde Schiff-base
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A new Schiff-base ligand (1) with good fluorescence response to Al 3+, derived from 2-oxo-quinoline-3-carbaldehyde and nicotinic hydrazide, had been synthesized and investigated in this paper. Spectroscopic investigation revealed that the compound 1 exhibited a high selectivity and sensitivity toward Al(III) ions over other commonly coexisting metal ions in ethanol, and the detection limit of Al3+ ions is at the parts per billion level. The mass spectra and Job's plot confirmed the 1:1 stoichiometry between 1 and Al3+. Potential utilization of 1 as intracellular sensors of Al3+ ions in human cancer (HeLa) cells was also examined by confocal fluorescence microscopy.
- Zhang, Ke,Yang, Zheng-Yin,Wang, Bao-Dui,Sun, Shao-Bo,Li, Ying-Dong,Li, Tian-Rong,Liu, Zeng-Chen,An, Jun-Mei
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- Design, synthesis, and evaluation of new 2-oxoquinoline arylaminothiazole derivatives as potential anticancer agents
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A series of novel 2-oxoquinoline derivatives containing arylaminothiazole were designed and synthesized as potential antitumor agents. The synthesized compounds were evaluated for their in vitro cytotoxicity activity against HeLa, NCI-H460, T24 and SKOV3
- Fang, Yilin,Wu, Zhilin,Xiao, Mengwu,Wei, Li,Li, Kangming,Tang, Yuting,Ye, Jiao,Xiang, Jiannan,Hu, Aixi
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- A Schiff's base receptor for red fluorescence live cell imaging of Zn2+ ions in zebrafish embryos and naked eye detection of Ni2+ ions for bio-Analytical applications
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An interesting dual chemoreceptor (QAMP) was synthesized to quantify the presence of two environmentally as well as biologically important Zn2+/Ni2+ ions in a highly selective manner using different analytical techniques. The fluorescence profile was enhanced to 663 nm (red region) due to the formation of its 1 : 1 complex with Zn2+ at room temperature even in the presence of other interfering ions such as Cd2+ and Hg2+. Moreover, it exhibits excellent chromo-isomerism with Ni2+ ions. Meanwhile, this assay could be successfully oriented with molecular logic functions of AND, OR, NOR and NOT logic gates. The obtained large Stokes shift (~274 nm) value and red emission promoted this receptor as a potential tool for biological studies (e.g. live cell imaging in cancer cell line and zebrafish models).
- Senthil Murugan,Vidhyalakshmi,Ramesh,Annaraj
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- Synthesis and photophysical investigation of 2-hydroxyquinoline-3-carbaldehyde: AIEE phenomenon, fluoride optical sensing and BSA interaction study
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Nowadays compounds showing aggregation-induced emission enhancement (AIEE) are extensively studied due to their huge range of applications in material science. AIEE and the anion recognition ability of 2-hydroxyquinoline-3-carbaldehyde (1) were explored. Unique AIEE phenomenon is observed in CH3CN with water as the cosolvent and the highest emission was noted in the solvent volume ratio 2:8 (CH3CN: H2O). The compound is a selective time dependent turn on fluoride ion sensor in acetonitrile medium with a distinct color change from colorless to yellow, fabricating it as a visible sensor. Ion sensing ability was monitored through UV–vis, steady state emission, life time studies and 1H NMR spectroscopy. The limit of detection of fluoride ion is 4.09 × 10?6 M. Moreover the compound exhibited notable quenching of fluorescence intensity with bovine serum albumin. Thus small molecule like the quinoline motif can be used in extensive applications in the scientific research.
- Chakraborty, Nilanjan,Bhuiya, Sutanwi,Chakraborty, Arijit,Mandal, Deep,Das, Suman
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- Chemistry of mixed-ligand oxidovanadium(IV) complexes of aroylhydrazones incorporating quinoline derivatives: Study of solution behavior, theoretical evaluation and protein/DNA interaction
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A series of eight hexacoordinated mixed-ligand oxidovanadium(IV) complexes [VO(Lx)(LN-N)] (1–8), where Lx = L1 – L4 are four differently substituted ONO donor aroylhydrazone ligands and LN-N are N,N-donor bases like 2,2′-bipyridine (bipy) (1, 3, 5 and 7) and 1,10-phenanthroline (phen) (2, 4, 6 and 8), have been reported. All synthesized complexes have been characterized by various physicochemical techniques and molecular structures of 1 and 6 were determined by X–ray crystallography. With a view to evaluate the biological activity of the VIVO species, the behavior of the systems VIVO2+/Lx, VIVO2+/Lx/bipy and VIVO2+/Lx/phen was studied as a function of pH in a mixture of H2O/DMSO 50/50 (v/v). DFT calculations allowed finding out the relative stability of the tautomeric forms of the ligands, and predicting the structure of vanadium complexes and their EPR parameters. To study their interaction with proteins, firstly the ternary systems VIVO2+/L1,2 with 1-methylimidazole, which is a good model for histidine binding, were examined. Subsequently the interaction of the complexes with lysozyme (Lyz), cytochrome c (Cyt) and bovine serum albumin (BSA) was studied. The results indicate that the complexes showed moderate binding affinity towards BSA, while no interaction takes place with lysozyme and cytochrome c. This could be explained with the higher number of accessible coordinating and polar residues for BSA than for Lyz and Cyt. Further, the complexes were also evaluated for their DNA binding propensity through UV–vis absorption titration and fluorescence spectral studies. These results were consistent with BSA binding affinity and showed moderate binding affinity towards CT-DNA.
- Banerjee,Dash, Subhashree P.,Mohanty, Monalisa,Sanna, Daniele,Sciortino, Giuseppe,Ugone, Valeria,Garribba, Eugenio,Reuter, Hans,Kaminsky, Werner,Dinda
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- Efficient synthesis of some pyrimidine and thiazolidine derivatives bearing quinoline scaffold under microwave irradiation
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An efficient and facile approach for the synthesis of new quinoline derivatives was accomplished via reactions of 2-chloroquinoline-3-carbaldehyde with active methylene compounds, for example, 1,3-dimethylbarbituric acid, thiobarbituric acid and 2,4-dioxo
- El-Naggar, Abeer M.,Ramadan, Sayed K.
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- Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or quinolone and thiazole moieties
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To develop novel antimicrobial agents, and based on the biologically active heterocyclic quinoline and thiazole substituted, a series of novel α-aminophosphonates (9a–h) and (10i–l) derivatives that incorporated quinoline or quinolone, and coumarylthiazole or 5-phenylthiazol-2-amine moieties were designed and synthesized via Kabachnik–Fields reaction in the presence of ionic liquid under ultrasound irradiation. All the new compounds were obtained in good yield with a simple workup and were confirmed using various spectroscopic methods. The in vitro antimicrobial activity of all synthesized compounds were screened in terms of MIC values against the selected strains of Gram-negative and Gram-positive bacteria and two fungal strains using the broth micro-dilution method. The results showed that most of the tested compounds showed moderate inhibitory activities against both Gram‐positive and ‐negative bacteria compared with reference drugs. The following compounds 9e, 9g, 9h, 9i and 9f, 9g, 9h, 10k, 10l are the most active against Gram-positive and Gram-negative bacteria strains, respectively, with MIC values ranging between 0.25 and 128 μg/mL. The synthesized compounds 9b, 9c, 9f, 9g, 9h, 10k, and 10l exhibited excellent antifungal inhibition with MIC values ranging between 0.25 and 32 μg/mL. Structure–activity relationship revealed that the presence of coumarylthiazole moiety and hydroxyl in the quinoline group increased the inhibitory activity against microbial strains pathogens. These results confirm that the synthesized compounds can be potential antimicrobial drugs candidate. [Figure not available: see fulltext.]
- Boukhari, Abbes,Djahoudi, Abdelghani,Litim, Bilal,Meliani, Saida
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- Potential antibacterial and antifungal activities of novel sulfamidophosphonate derivatives bearing the quinoline or quinolone moiety
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A series of new α-sulfamidophosphonate/sulfonamidophosphonate (4a–n) and cyclosulfamidophosphonate (5a–d) derivatives containing the quinoline or quinolone moiety was designed and synthesized via Kabachnik–Fields reaction in the presence of ionic liquid under ultrasound irradiation. This efficient methodology provides new 1,2,5-thiadiazolidine-1,1-dioxide derivatives 5a–d in one step and optimal conditions. The molecular structures of the novel compounds 4a–n and 5a–d were confirmed using various spectroscopic methods. All these compounds were evaluated for their in vitro antibacterial activity against Gram-negative (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853) and Gram-positive (Staphylococcus aureus ATCC 27923) bacteria, in addition to three clinical strains (E. coli 1, P. aeruginosa 1, and S. aureus 1). Most of the tested compounds showed more potent inhibitory activities against both Gram-positive and -negative bacteria compared with the sulfamethoxazole reference. The following compounds, 4n, 4f, 4g, 4m, 4l, 4d, and 4e, are the most active sulfamidophosphonate derivatives. Furthermore, these molecules gave interesting zones of inhibition varying between 28 and 49 mm, against all tested bacterial strains, with a low minimum inhibitory concentration (MIC) value ranging from 0.125 to 8 μg/ml. All the synthesized derivatives were also evaluated for their in vitro antifungal activity against Fusarium oxyporum f. sp. lycopersici and Alternaria sp. The results revealed that all the synthesized compounds exhibited excellent antifungal inhibition and the compounds 4f, 4g, 4m, and 4i were the most potent derivatives with MIC values ranging from 0.25 to 1 μg/ml against the two tested fungal strains. The strongest inhibition of bacteria and fungi strains was detected by the effect of quinolone and sulfamide moieties.
- Bazine, Ismahene,Bendjedid, Samira,Boukhari, Abbes
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- New 3-(1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one-based triazole derivatives: Design, synthesis, and biological evaluation as antiproliferative and apoptosis-inducing agents
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A series of 1,2,3-triazole derivatives based on the quinoline–benzimidazole hybrid scaffold was designed, synthesized, and screened against a panel of NCI-60 humanoid cancer cell lines for in vitro cytotoxicity evaluation, which revealed that compound Q6 was the most potent cytotoxic agent with excellent GI50, TGI, and LC50 values on multiple cancer cell lines. Q6 was tested further on the BT-474 breast cancer line to evaluate the mechanism of action. Preliminary screening studies based on the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay revealed that compound Q6 had an excellent antiproliferative effect against human breast cancer cells, BT-474, with IC50 values of 0.59 ± 0.01 μM. The detailed study based on the acridine orange/ethidium bromide staining (AO/EB) and the 4′,6-diamidino-2-phenylindole (DAPI) assay suggested that the antiproliferative activity shown was due to the induction of apoptosis on exposure to Q6. Further, DCFDA staining showed the generation of reactive oxygen species, altering the mitochondrial potential and leading to the initiation of apoptosis. This was further supported by JC-1 staining, indicating that this scaffold can contribute to the development of more potent derivatives.
- Gaikwad, Nikhil B.,Bansode, Sapana,Biradar, Shankar,Ban, Mayuri,Srinivas, Nanduri,Godugu, Chandraiah,Yaddanapudi, Venkata M.
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- Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors
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The targeted approach of protein kinases (PKs), as PKs are the main regulators of cell survival and proliferation, has been a promising strategy for cancer treatments. Here we analyse the potential of quinoline-carboxamide derivatives for four cell lines: MCF-7, CACO, HepG-2 and HCT-116 as anticancer agents. 3e, 4b, 11b and 13d derivatives showed good anti-proliferative activities in comparison to the reference standard Doxorubicin, against the four cell lines tested. They have been chosen for further studies. First of all, the IC50 value surveys were carried out to ensure the protection of our hits and demonstrate that the cytotoxic effect (IC50 > 113 μM) is highly selective on normal human cells (WI-38). Secondly, apoptosis was accomplished by down-regulation of Bcl-2 and up-regulation of BAX and Caspase-3 by these active compounds. Also, the Pim-1 inhibitory activity of the active hybrids was done, which indicates that compound 3e was the most active with the percentage of inhibition 82.27% and IC50 equals 0.11 when compared to SGI-1776 as a reference standard. In addition, by in silico assessment of ADME properties, all of the strongest compounds are orally bioavailable without blood–brain barrier penetration. [Figure not available: see fulltext.].
- Abusaif, Moustafa S.,Ammar, Yousry A.,Elhagali, Gamil A. M.,Fayed, Eman A.,Mehany, Ahmed B. M.,Naser, Tamer,Selim, Mohamed R.,Zahran, Medhat A.
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p. 1649 - 1668
(2021/08/16)
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- Synthesis, photophysical properties and theoretical studies of new bis-quinolin curcuminoid BF2-complexes and their decomplexed derivatives
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This paper presents the synthesis and characterization of two series of new bis-quinolin curcuminoid BF2-complexes 11 and their respective decomplexed bis-quinolin curcuminoid derivatives 12, in an attempt to understand their optical properties. The synthesized compounds showed interesting fluorescent characteristics in both solution and in solid-state. The characteristic of the electronic transitions involved in these systems were measured via Uv-vis spectroscopy and fluorescence spectroscopy. Results revealed that the absorption and emission bands are dependent of the structure of compounds 11 and 12 but also of the type of substituent, even showing a push-pull behavior in those derivatives substituted with methyl group. These findings were also confirmed through computational calculations at DFT level via simulations of the Uv-vis spectra and determining the topology of the border orbitals responsible for light absorption.
- Abonia, Rodrigo,Cabrera, Lorena,Insuasty, Braulio,Insuasty, Daniel,Ortiz, Alejandro,Quiroga, Jairo
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- Synthesis, antioxidant and anticholinesterase activities of novel quinoline-aminophosphonate derivatives
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A series of 20 novel α-aminophosphonate derivatives bearing quinoline or quinolone moiety was designed and synthesized via Kabachnik-Fields reaction in the presence of triethylammonium acetate as a solvent and catalyst under ultrasound irradiation. This procedure affords products in high yields and short reaction times. Molecular structures of the synthesized compounds 4a-g and 5a-m were confirmed using various spectroscopic methods. The antioxidant activity of these compounds was evaluated by eight complementary in vitro tests. The anticholinesterase activity (AChE, BChE) of these compounds were also evaluated. In addition, theoretical calculations of all compounds were investigated as corrosion inhibitors using density functional theory (DFT). The results revealed that 16 of these compounds exhibited high levels of antioxidant activities depending on the assay and that most compounds showed more potent inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
- Bazine, Ismahene,Bensegueni, Rafik,Bensouici, Chawki,Boukhari, Abbes,Cheraiet, Zinelaabidine
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- Synthesis, molecular docking and antimicrobial activities of 3-formyl-2-(1h)quinolinone schiff base derivatives and 3-(((3-acetylphenyl)imino)- methyl)quinolin-2-(1h)-one chalcone derivatives
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Some of Schiff base derivatives were separated by condensing 3-formyl-2-quinolinone with various primary amine derivatives in ethanol, in which water is expelled. Moreover, substituted acryloylphenyliminomethylquinolinone chalcone derivatives were prepared by the process of condensation reaction of aldehyde derivatives with 3-acetylphenylquinolinone in dilute solution of ethanolic sodium hydroxide via Claisen-Schmidt condensation method. Cyclization reaction of the quinolinone chalcones with malononitrile, phenylhydrazine, urea and thiourea were also investigated. The structures of these compounds have been elucidated on the bases of spectral data. The novel products were also evaluated for their antimicrobial activity.
- Maigali,Tawfik,Abd-El-Maksoud,Soliman,Moharam,Dondeti
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p. 3903 - 3914
(2020/11/18)
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- CRBN LIGANDS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
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- Novel quinoline derivatives carrying nitrones/oximes nitric oxide donors: Design, synthesis, antiproliferative and caspase-3 activation activities
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Novel quinoline derivatives carrying nitrones and oxime as nitric oxide donors were prepared and characterized using different spectroscopic techniques. Nitrones can release nitric oxide in larger amounts compared to corresponding oximes. Antiproliferativ
- Abdelbaset, Mahmoud S.,Abdel-Aziz, Mohamed,Abuo-Rahma, Gamal El-Din A.,Abdelrahman, Mostafa H.,Ramadan, Mohamed,Youssif, Bahaa G. M.
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- Synthesis, antibacterial activity and docking studies of substituted quinolone thiosemicarbazones
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Fifteen 2-quinolone thiosemicarbazone derivatives of which eleven were new, were synthesized at room temperature. The key intermediate was the quinolone carbaldehyde, from which thiosemicarbazones were formed by the reaction of thiosemicarbazides with the aldehyde moiety. The structures of the synthesized compounds were elucidated by 1D and 2D-NMR spectroscopy and mass spectrometry. The synthesized compounds showed antibacterial activity with MBCs in the range 0.80 to 36.49 mM against Staphylococcus aureus, Staphylococcus aureus Rosenbach (MRSA), Pseudomonas aeruginosa, Klebsiella pneumoniae, Escherichia coli and Salmonella typhimurium. The best activity was seen when a larger halogen such as chlorine and bromine were substituted at C-6 on the quinolone scaffold and when a planar phenyl group was present on the thiosemicarbazone moiety. Activity was reduced when a smaller fluorine atom was present at C-6 or when a methyl group was attached to the thiosemicarbazone. This group of compounds showed a high negative binding affinity, which suggested promising antimcrobial activity. The 6-chloro derivative with a phenyl group on the thiosemicarbazone had the greatest negative binding affinity.
- Govender, Hogantharanni,Mocktar, Chunderika,Kumalo, Hezekiel M.,Koorbanally, Neil A.
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p. 1074 - 1081
(2019/06/10)
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- Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
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Eight quinoline-based hydroxyimidazolium hybrids 7a-h were prepared and evaluated in vitro against a panel of clinically important fungal and bacterial pathogens, including mycobacteria. Hybrid compounds 7c-d showed remarkable antifungal activity against Cryptococcus neoformans with a minimum inhibitory concentration (MIC) value of 15.6 μg/mL. Against other opportunistic fungi such as Candida spp. and Aspergillus spp., these hybrids showed MIC values of 62.5 μg/mL. Regarding their antibacterial activity, all the synthetic hybrids demonstrated little inhibition of Gram-negative bacteria (MIC ≥50 μg/mL), however, hybrid 7b displayed >50% inhibition against Klebsiella pneumoniae at 20 μg/mL and full inhibition at 50 μg/mL. Moreover, this hybrid was shown to be a potent anti-staphylococcal molecule, with a MIC value of 2 μg/mL (5 μM). In addition, hybrid 7h also demonstrated inhibition of Staphylococcus aureus at 20 μg/mL (47 μM). Hybrids 7a and 7b were the most potent against Mycobacterium tuberculosis H37Rv with MIC values of 20 and 10 μg/mL (46 and 24 μM), respectively. The 7b hybrid demonstrated high selectivity in killing S. aureus and M. tuberculosis H37Rv in comparison with mammalian cells (SI >20), and thus it can be considered a hit molecule for mechanism of action studies and the exploration of related chemical space.
- Abonia, Rodrigo,Bernal, Anthony,Guzman, Juan,Insuasty, Braulio,Insuasty, Daniel,Marquez, Edgar,Puerto, Gloria,Quiroga, Jairo,Svetaz, Laura,Vidal, Oscar,Zacchino, Susana
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- FLUORESCENT DYE AGENT AND CARBOSTYRIL COMPOUND
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PROBLEM TO BE SOLVED: To provide a novel fluorescent dye agent. SOLUTION: A fluorescent dye agent contains a carbostyril compound represented by formula (1) [in the formula (1), R1 is H, a halogen atom, a hydroxyl group, a cyano group, a nitro group or the like; R2 is O; R3 is a halogen atom, a carboxyl group, an ester group, an amide group or the like; R4-R6 and R8 independently represent H, a halogen atom, a nitro group, a cyano group or the like, where mutually adjacent groups of R4-R8 may be bound to form a ring; R7 is H, a substituted or unsubstituted aliphatic group or the like]. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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- Catalyst-free assembly of giant tris(heteroaryl)methanes: Synthesis of novel pharmacophoric triads and model sterically crowded tris(heteroaryl/aryl)methyl cation salts
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A series of giant tris(heteroaryl)methanes are easily assembled by one-pot three-component synthesis by simple reflux in ethanol without catalyst or additives. Diversely substituted indoles (Ar1) react with quinoline aldehydes, quinolone aldehydes, chromone aldehydes, and fluorene aldehydes (Ar2CHO) and coumarins (Ar3) in 1:1:1 ratio to form the corresponding tris(heteroaryl)methanes (Ar1Ar2Ar3)CH along with (Ar1Ar1Ar2)CH triads. A series of new 2:1 triads were also synthesized by coupling substituted indoles with Ar2CHO. The coupling reactions could also be carried out in water (at circa 80 °C) but with chemoselectivity favoring (Ar1Ar1Ar2)CH(Ar1Ar2Ar3)CH. The molecular structure of a representative (Ar1Ar2Ar3)CH triad was confirmed by X-ray analysis. Model tris(heteroaryl/aryl)methylium salts were generated by reaction with DDQ/HPF6 and studied by NMR and by DFT and GIAO-DFT.
- Abonia, Rodrigo,Gutiérrez, Luisa F.,Insuasty, Braulio,Quiroga, Jairo,Laali, Kenneth K.,Zhao, Chunqing,Borosky, Gabriela L.,Horwitz, Samantha M.,Bunge, Scott D.
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p. 642 - 654
(2019/04/17)
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- Design of new quinolin-2-one-pyrimidine hybrids as sphingosine kinases inhibitors
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Sphingosine-1-phosphate is now emerging as an important player in cancer, inflammation, autoimmune, neurological and cardiovascular disorders. Abundance evidence in animal and humans cancer models has shown that SphK1 is linked to cancer. Thus, there is a
- Abonia, Rodrigo,Andújar, Sebastián,Cobo, Justo,Enriz, Ricardo D.,Gutiérrez, Lucas,Insuasty, Daniel,Lima, Santiago,Marchal, Antonio,Nogueras, Manuel,Spiegel, Sarah,Vettorazzi, Marcela
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- Preparation and characterization of rod-like chitosan–quinoline nanoparticles as pH-responsive nanocarriers for quercetin delivery
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Novel chitosan–quinoline nanoparticles as anticancer drug nanocarriers were prepared using 2-chloro-3-formylquinoline and 3-formylquinolin-2(1H)-one as non-toxic modifying agents via oil–in–water nanoemulsion technique. Chitosan–quinoline nanoparticles were characterized by FT–IR, UV–vis spectrophotometry, XRD, SEM, AFM and DLS techniques. The morphological and particle size studies demonstrated that drug–loaded chitosan–quinoline nanoparticles have a regular nanorod shape and monolithic structure with the desired particle size of 141 to 174.8 nm and a negative zeta potential of ?2.4 to ?14.1 mV. Drug loading capacity (LC) and encapsulation efficiency (EE) were achieved using quercetin as a hydrophobic anticancer drug and were about 4.8–9.6% and 65.8–77%, respectively. The in vitro release studies displayed great pH-sensitive release behavior. Evaluation of the anticancer efficacy of quercetin loaded chitosan–quinoline nanoparticles using the in vitro cytotoxicity studies against HeLa cells indicated that the chitosan nanoparticles are a promising candidate for the anticancer drugs delivery.
- Rahimi, Shahnaz,Khoee, Sepideh,Ghandi, Mehdi
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p. 279 - 289
(2019/02/03)
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- Synthesis, antiplasmodial and antitrypanosomal evaluation of a series of novel 2-oxoquinoline-based thiosemicarbazone derivatives
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Herein a series of novel thiosemicarbazones (TSCs) derived from 2-oxoquinoline scaffold is reported, and the target compounds have been successfully synthesized and characterized using standard spectroscopic techniques. The in vitro biological activities of synthesized molecules were evaluated against Plasmodium falciparum malaria parasites (strain 3D7), Trypanosoma brucei brucei parasites (strain 427) and HeLa cells. All the compounds displayed modest or no activity at a concentration of 20 μM and percentage viability of >50 % was often observed. Except for compound 9o, none of the final compounds exhibited cytotoxic effects against HeLa cells at 20 μM.
- Darrell, Oliver T.,Hulushe, Siyabonga T.,Mtshare, Thanduxolo E.,Beteck, Richard M.,Isaacs, Michelle,Laming, Dustin,Hoppe, Heinrich C.,Krause, Rui W.M.,Khanye, Setshaba D.
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p. 174 - 181
(2019/01/04)
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- Design, synthesis and pharmacological evaluation of new 3-(1H-benzimidazol-2-yl)quinolin-2(1H)-one derivatives as potential antitumor agents
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A series of new 3-(1H-benzimidazol-2-yl)quinolin-2(1H)-one derivatives (5a1?5d6) were designed and synthesized as antitumor agents. In vitro antitumor assay results showed that some compounds exhibited moderate to high inhibitory activity against HepG2, SK-OV-3, NCI-H460 and BEL-7404 tumor cell lines, and most compounds exhibited much lower cytotoxicity against the HL-7702 normal cell line compared to 5-FU and cisplatin. In vivo antitumor assay results demonstrated that 5a3 exhibited effective inhibition on tumor growth in the NCI-H460 xenograft mouse model and that 5d3 displayed excellent antiproliferative activity in the BEL-7402 xenograft model. These results suggested that both 5a3 and 5d3 could be used as anticancer drug candidates. Mechanistic studies suggested that compounds 5a3 and 5d3 exerted their antitumor activity by up-regulation of Bax, intracellular Ca2+ release, ROS generation, downregulation of Bcl-2, activation of caspase-9 and caspase-3 and subsequent cleavage of PARP, inhibition of CDK activity and activation of the p53 protein.
- Kuang, Wen-Bin,Huang, Ri-Zhen,Qin, Jiao-Lan,Lu, Xing,Qin, Qi-Pin,Zou, Bi-Qun,Chen, Zhen-Feng,Liang, Hong,Zhang, Ye
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p. 139 - 150
(2018/08/09)
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- Microwave-assisted synthesis of diversely substituted quinoline-based dihydropyridopyrimidine and dihydropyrazolopyridine hybrids
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An efficient, catalyst-free, and one-pot three-component procedure for the synthesis of novel and nitrogen rich dihydropyrido[2, 3-d]pyrimidines and dihydro-1H-pyrazolo[3, 4-b]pyridines bearing a quinoline pharmacophore fragment is provided. Reactions proceeded in DMF under microwave irradiation of three-component mixtures of formyl-quinoline derivatives, primary heterocyclic amines and cyclic 1, 3-diketones. Interestingly, when conventional heating at reflux was used for the starting 5-amino-1-phenylpyrazole, the corresponding aromatized pyrazolopyridines were obtained as the main products. Single crystal X-ray analysis confirmed unequivocally the structure of both the dihydro- and aromatized products.
- Insuasty, Daniel,Abonia, Rodrigo,Insuasty, Braulio,Quiroga, Jairo,Laali, Kenneth K.,Nogueras, Manuel,Cobo, Justo
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p. 555 - 563
(2017/10/13)
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- A mixed-valence metallogrid [CoIII2CoII2] with an unusual electronic structure and single-ion-magnet characterization
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The reaction of the multisite coordination ligand (H2L) with Co(Ac)2·4H2O in the absence of any base affords a homometallic tetranuclear mixed-valence complex, [Co4(L)4(CH3CO2)s
- Huang, Wei,Pan, Feifei,Wang, Zhenxing,Bai, Yan,Feng, Xuejun,Gu, Jiande,Ouyang, Zhong-Wen,Wu, Dayu
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p. 5069 - 5075
(2017/04/17)
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- Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents
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A series of novel 2-oxo-quinoline derivatives containing α-aminophosphonates were designed and synthesized as antitumor agents. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay results demonstrated that some compounds exhibited moderate to high inhibitory activity against HepG2, SK-OV-3 and NCI-H460 tumor cell lines, and most compounds showed much lower cytotoxicity against HL-7702 normal cells than 5-FU and cisplatin. The action mechanism of representative compound 5b was investigated by fluorescence staining assay, flow cytometric analysis and western blot (WB) assay, which indicated that this compound induced apoptosis and G2/M phase arrest accompanied by an increase in the production of intracellular Ca2+ and reactive oxygen species (ROS) and affecting associated enzymes and genes.
- Yu, Yan-Cheng,Kuang, Wen-Bin,Huang, Ri-Zhen,Fang, Yi-Lin,Zhang, Ye,Chen, Zhen-Feng,Ma, Xian-Li
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p. 1158 - 1172
(2017/07/07)
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- A Schmidt rearrangement-mediated synthesis of novel tetrahydro-benzo[1,4]diazepin-5-ones as potential anticancer and antiprotozoal agents
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Novel tetrahydro-5H-benzo[e][1,4]diazepin-5-ones, several of them, containing the quinoline pharmacophore, were synthesized via a Schmidt rearrangement from their corresponding 1,2,3,4-tetrahydro-4-quinolones mediated by the NaN3/H2SO4 reaction conditions. Twelve of the obtained compounds were in vitro screened by the US National Cancer Institute (NCI) for their ability to inhibit 60 different human tumor cell lines, where compound 24a presented a remarkable activity against 58 of the 60 cancer cell lines, with the most important GI50 values ranging from 0.047 to 8.16 μM and LC50 values ranging from 9.4 to > 100 μM. Additionally, some of them were evaluated as antimalarial, antitrypanosomal and antileishmanial agents. The best antimalarial response was observed for compound 22g with an EC50 = 13.61 μg/mL for Plasmodium falciparum, while compound 24d exhibited high activity against Trypanosoma cruzi. and Leishmania (V) panamensis with EC50 = 2.78 μg/mL and 3.35 μg/mL respectively.
- Insuasty, Daniel,Robledo, Sara M.,Vélez, Iván D.,Cuervo, Paola,Insuasty, Braulio,Quiroga, Jairo,Nogueras, Manuel,Cobo, Justo,Abonia, Rodrigo
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p. 567 - 583
(2017/11/03)
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- Synthesis and anticonvulsant activity of a combined pharmacophore of 2-oxo-1,2-dihydroquinoline containing 1,3,4-oxadiazole derivatives
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The significance of 1,3,4-oxadiazolo-quinoline as pharmacophore in the discovery of better antiepileptic agent led to the exploration of the synthesis of new series of 3-[5-(naphthyloxymethyl/naphthyl-methyl/2-phenoxymethyl) benzoimidazol-1-ylmethyl)-[1,3
- Salahuddin,Mazumder, Avijit,Yar, Mohammad Shahar,Sarafroz, Mohammad
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- Synthesis, characterization and antimicrobiolgical activity of schiff bases derived from 2- hydroxyquinoline-3-carbaldehydes
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A series of six new N-[(2-hydroxy-quinolin-3-yl)methlidene]benzohydrazides (1-6) has been synthesized by the condensation of 2-hydroxy-quinoline-3-carbaldehydes with benzohydrazide derivatives. The newly synthesized compounds displayed hydrogen bonding as
- Mallandur, Bhargava K.,Rangaiah, Gururaja,Harohally, Nanishankar V.
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- Application of [2-(1H)-quinolinone-3-yl]naphthalenyl aminomethyl phosphonate as anti-cancer drug
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The invention discloses [2-(1H)-quinolinone-3-yl]naphthalenyl aminomethyl phosphonate shown in the structural formula I (please see the formula in the description) and pharmaceutically-acceptable salt of [2-(1H)-quinolinone-3-yl]naphthalenyl aminomethyl phosphonate. R is selected from C1-C2 alkyl groups, C3-C4 linear alkyl groups or branched alkyl groups, and X1-X8 are each selected from hydrogen, deuterium and C1-C2 alkyl groups. The invention discloses [2-(1H)-quinolinone-3-yl]naphthalenyl aminomethyl phosphonate, the pharmaceutically-acceptable salt of [2-(1H)-quinolinone-3-yl]naphthalenyl aminomethyl phosphonate and application of a medicine composition in preparation of anti-cancer drugs.
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Paragraph 0030; 0031
(2016/10/27)
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- Application of [2-(1H)-quinolinone-3-yl]phenylamino methylphosphonate as anti-cancer drug
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The invention discloses [2-(1H)-quinolinone-3-yl]phenylamino methylphosphonate shown in the structural formula I and pharmaceutically-acceptable salt (please see the formula in the description) of [2-(1H)-quinolinone-3-yl]phenylamino methylphosphonate. R is selected from an alkyl group of C1-C2, a gaseous normal alkyl group of C3-C4 and a branched alkyl group; X1 and X2 are selected from hydrogen, deuterium and an alkyl group of C1-C2; X3 and X7 are selected from hydrogen, deuterium, an alkyl group of C1-C2, fluorine, chlorine, bromine, iodine and a nitryl group; X4 and X6 are selected from hydrogen, deuterium, a trifluoromethyl group, an alkyl group of C1-C2, fluorine, chlorine, bromine and iodine; X5 is selected from hydrogen, deuterium, a trifluoromethyl group, an alkyl group of C1-C2, an alkoxy group of C1-C2, fluorine, chlorine, bromine, iodine and a nitryl group. The invention discloses application of [2-(1H)-quinolinone-3-yl]phenylamino methylphosphonate, the pharmaceutically-acceptable salt and a medicine composition of [2-(1H)-quinolinone-3-yl]phenylamino methylphosphonate in the preparation of anti-cancer drug.
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Paragraph 0030; 0031
(2016/10/24)
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- Design, Synthesis, and Evaluation of 3-((4-(t-Butyl)-2-(2-benzylidenehydrazinyl)thiazol-5-yl)methyl)quinolin-2(1H)-ones as Neuraminidase Inhibitors
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A series of novel 3-((4-(t-butyl)-2-(2-benzylidenehydrazinyl)thiazol-5-yl)methyl)quinolin-2(1H)-ones (7a-7z) were designed, synthesized and evaluated for their ability of inhibiting neuraminidase (NA) of in?uenza H1N1 virus. Some compounds displayed moder
- Fang, Yilin,Xiao, Mengwu,Hu, Aixi,Ye, Jiao,Lian, Wenwen,Liu, Ailin
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p. 403 - 411
(2016/04/26)
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- 3-benzimidazole -2 (1H)-Quinolinone derivative and its preparation method and application (by machine translation)
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The present invention discloses a kind of 3-benzimidazole -2 (1H)-Quinolinone derivative and its preparation method and application. The preparation process of the derivative for the: heating 2 (1H)-Quinolinone derivatives and O-phenylene diamine derivatives soluble in organic solvent, the reaction is carried out under heating condition, to obtain. With commonly used anti-tumor drug 5-FU and compared with platinum, the derivative of the invention in the activity of certain derivatives of the more efficient, the normal human liver cell HL-7702 low toxicity. The invention the 3-benzimidazole -2 (1H)-Quinolinone derivative has if following type (I) the structure shown in: wherein R 1 is hydrogen, methyl, methoxy or R 2 form a 1,2-methylene-dioxy; R 2 is hydrogen or R 1 form a 1,2-methylene-dioxy; R 3 is hydrogen, methyl, methoxy, fluoro, chlorine-based, bromo, nitro or trifluoromethyl; R 4 is hydrogen, methyl, methoxy or chlorine-based. (by machine translation)
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- Molecular and Nanoaggregation in Cyclometalated Iridium(III) Complexes through Structural Modification
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New terpyridyl ligands TP1, TP2 and cyclometalated iridium(III) complexes 1 and 2 based on these ligands have been synthesized. The ligands and complexes have been characterized by elemental analysis and spectroscopic studies (ESI-MS,1H and13C NMR, UV/Vis, fluorescence). The molecular structure of 1 has been verified by X-ray single-crystal analysis. It has been unambiguously established that variation of the substituents on 1 and 2 leads to molecular aggregation in 1, while 2 remains nonaggregated. Furthermore, complexes 1 and 2 have been successfully utilized as capping agents for the stabilization of gold nanoparticles (AuNPs). It is of note that 1 forms discretely, while 2 aggregates AuNPs through the assemblage of ultrasmall nanoparticles. It has been affirmed by1H NMR titration studies that –NH groups from 1 and 2 are involved in the capping of AuNPs. The role of simple structural variations in directing molecular and nanoaggregation has been clearly established for the first time by spectroscopic (UV/Vis, fluorescence,1H NMR titration) and morphological studies [SEM, TEM, EDX (energy-dispersive X-ray), DLS (dynamic light scattering)].
- Mukhopadhyay, Sujay,Singh, Roop Shikha,Biswas, Arnab,Maiti, Biswajit,Pandey, Daya Shankar
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p. 4199 - 4206
(2016/09/16)
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- Synthesis and anticancer activity of novel curcumin-quinolone hybrids
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A number of new curcumin-quinolone hybrids were synthesised from differently substituted 3-formyl-2-quinolones and vanillin and their in vitro cytotoxicity was determined on a panel of representative cell lines (A549, MCF7, SKOV3 and H460) using MTT assay. The most potent compound 14, was analysed for its mode of action using various cell biology experiments. SKOV3 cells treated with compound 14 showed distorted cell morphology under phase contrast imaging and induction of apoptosis was confirmed by Annexin V/PE assay. Further experiments on generation of reactive oxygen species (ROS) and cell cycle analysis revealed that these hybrids induce apoptosis by ROS generation and arrest cell cycle progression in S and G2/M phase.
- Raghavan, Saiharish,Manogaran, Prasath,Gadepalli Narasimha, Krishna Kumari,Kalpattu Kuppusami, Balasubramanian,Mariyappan, Palanivelu,Gopalakrishnan, Anjana,Venkatraman, Ganesh
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p. 3601 - 3605
(2015/08/11)
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- Synthesis, antibacterial and antitubercular activities of some novel quinoline derivatives
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6-Substituted/unsubstituted-2-chloro-3-formylquinolines 1(a,b) were synthesized by Vilsmeier-Haack reaction. These compounds on microwave irradiation with 4M HCl yielded 6-substituted/unsubstituted-2-hydroxy quinoline-3-carbaldehydes 2(a,b). These resulting compounds on treatment with different substituted hydrazides yielded the Schiff bases 3(a-j). The structures of all newly synthesized compounds were confirmed by spectral study such as IR and 1H NMR spectroscopy. All the synthesized compounds were screened for antibacterial and antitubercular activities. For antibacterial activity MIC values for the synthesized compounds were determined using serial dilution method and ciprofloxacin and norfloxacin were used as standard drugs and for antitubercular activity the synthesized compounds were screened against Mycobacterium tuberculosis strain H37Rv using the Microplate Alamar Blue Assay (MABA) method using isoniazid as the standard drug. Compounds 3a, 3c, 3e, 3g and 3j showed significant antibacterial activity and compounds 3c, 3g and 3j showed good antitubercular activity.
- Kumar, M.R. Pradeep,Joshi,Dixit,Kulkarni
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p. 353 - 358
(2019/01/21)
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- Synthesis of new biphenyl-substituted quinoline derivatives, preliminary screening and docking studies
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New quinoline derivatives containing biphenyl ring were synthesized and characterized by IR, 1H NMR and mass spectral studies. The synthesized compounds were screened for antimicrobial, anthelmintic activities as well as free radical scavenging property against the DPPH radical. The minimum inhibition concentration values showed promising inhibiting activity and are potent biological agents. The compounds showed minimum binding energy towards ?-tubulin. The compounds 11a, 11c, 13c and 13d have good affinity towards the active pocket and may be considered as a good inhibitor of β-tubulin. Indian Academy of Sciences.
- Shashikumar, Nellisara D.,Krishnamurthy, Ganganaika,Bhojyanaik, Halehatti S.,Lokesh, Mayasandra R.,Jithendrakumara, Kaginalli S.
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p. 205 - 212
(2014/04/03)
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- Novel quinoline-imidazolium adducts via the reaction of 2-oxoquinoline-3-carbaldehyde and quinoline-3-carbaldehydes with 1-butyl-3-methylimidazolium chloride [BMIM][Cl]
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A library of hydroxyquinolin-3-ylmethylimidazolium adducts were prepared in high yields from the reaction of [BMIM][Cl] with various substituted quinoline-3-carbaldehydes and 2-oxoquinoline-3-carbaldehydes under mild conditions by using sodium acetate in MeCN under ultrasound irradiation. The use of sodium acetate and imidazolium chloride was crucial for the success of these CC bond forming reactions. Attempted coupling with thiazolium bromide led instead to quinoline-3-carboxylic acid.
- Laali, Kenneth K.,Insuasty, Daniel,Abonia, Rodrigo,Insuasty, Braulio,Bunge, Scott D.
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p. 4395 - 4399
(2014/07/22)
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- Solvent-free, one-pot synthesis and biological evaluation of some new dipyrazolo [3,4-b:4′,3′-e]pyranylquinolones and their precursors
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One-pot synthesis of 24 new compounds, belonging to three families; dipyrazolo[3,4-b:4′,3′-e]pyranylquinolones 7a-h and its precursors (pyrazolonylidene)methylquinolones 5a-h and 4,4′-[(quinolinyl)methylene] bispyrazols 6a-h, 8 from each, has been achieve
- Parmar, Narsidas J.,Pansuriya, Bhavesh R.,Parmar, Bhagyashri D.,Barad, Hitesh A.
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- Synthesis of some new pyrano[2,3-b]quinolines from 2-chloro-3-formylquinolones and Meldrum's acid
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A new series of functionalized pyrano[2,3-b]quinolines have been prepared in three steps from first condensation of 3-formyl-2-quinolones with Meldrum's acid, then the corresponding olefins have been alkylated using methyl magnesium iodide, and finally the target compounds have been obtained in good yields after hydrolysis.
- Guenfoud, Fatiha,Boulcina, Raouf,Laabassi, Mohammed,Mosset, Paul
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p. 736 - 742
(2015/04/14)
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- Synthesis and antitumor activities of some 2-oxo-quinoline-3-Schiff base derivatives
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A series of 2-oxo-quinoline-3-Schiff-base derivatives (4a1-4n2) have been designed and synthesized as new antitumor agents. in vitro Antitumor activities were evaluated against four cancer cell lines including MGC80-3, BEL-7404, A549 and NCI-H460. Compounds 4a1, 4a2, 4c2, 4d1, 4d2 and 4l2 exhibited better inhibition activities than commercial antitumor drug 5-fluorouracil (5-fluorouracil, IC50 = 44 ±0.54 μM) on NCI-H460, with IC50 of 35.52 ± 0.86, 16.22 ± 0.71, 11.62 ± 0.52, 5.16 ± 0.37, 7.62 ± 0.46 and 7.66 ± 0.65 μM, respectively.
- Fang, Yilin,Yi, Xianghui,Qin, Wen,Zhang, Ye,Liao, Yongzhi
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p. 7449 - 7451
(2015/04/22)
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- Synthesis of new biphenyl-substituted quinoline derivatives, preliminary screening and docking studies
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New quinoline derivatives containing biphenyl ring were synthesized and characterized by IR, 1H NMR and mass spectral studies. The synthesized compounds were screened for antimicrobial, anthelmintic activities as well as free radical scavenging property against the DPPH radical. The minimum inhibition concentration values showed promising inhibiting activity and are potent biological agents. The compounds showed minimum binding energy towards β-tubulin. The compounds 11a, 11c, 13c and 13d have good affinity towards the active pocket and may be considered as a good inhibitor of β-tubulin.
- Shashikumar, Nellisara D,Krishnamurthy, Ganganaika,BhojyaNaik, Halehatti S,Lokesh, Mayasandra R,Jithendrakumara, Kaginalli S
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p. 205 - 212
(2016/03/01)
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- Synthesis and antioxidant activities of 2-oxo-quinoline-3-carbaldehyde Schiff-base derivatives
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A series of 2-oxo-quinoline-3-carbaldehyde Schiff-base derivatives 4a 1-4n2 were designed and synthesized based on the 2-oxo-quinoline structure core as novel antioxidants. In vitro antioxidant activities of these compounds were evaluated and compared with commercial antioxidants ascorbic acid, BHT and BHA, employing DPPH assay, ABTS+ assay, O2- assay and OH assay. The results showed that IC50 of most compounds were lower than standard value 10 mg/mL, indicating good antioxidant activities of these compounds. In addition, in vitro antioxidant activities screening revealed that 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities of compounds 4b2, 4e 1, 4e2 and 4g2, 2,2′-azinobis-(3- ethylbenzthiazoline-6-sulphonate) cation (ABTS+) radical scavenging activities of compounds 4a1, 4e1, 4e2, 4f 1, 4f2, 4g1, 4g2, 4h1, 4h2, 4k1, 4k2, 4n1 and 4n 2, superoxide anion radical scavenging activities of 4b1, 4e1, 4f2, 4j1, 4k1, 4k2, 4m1, 4m2, and 4n2, and hydroxyl radical scavenging activity of almost all the compounds except 4f1, 4f 2, 4j2, 4l1 and 4l2 were better than that of the commercial antioxidant butylated hydroxytoluene (BHT).
- Zhang, Ye,Fang, Yilin,Liang, Hong,Wang, Hengshan,Hu, Kun,Liu, Xianxian,Yi, Xianghui,Peng, Yan
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p. 107 - 111
(2013/02/23)
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- An efficient synthesis of quinalone-3-(N-phenylpyrazoles) and quinalone-3-cyclohexadienone derivatives
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An efficient synthesis of quinalone-3-(N-phenylpyrazoles) 5 and quinalone-3-(cyclohexadienones) 8 has been described. 2-Chloroquinoline-3- carboxaldehyde 1, on reaction with 4N HCl gives 3-formyl-2(1H)-quinalone 2. The latter is reacted with acetophenone
- Praveen Kumar Darsi,Shiva Kumar,Rama Devi,Naidu,Dubey
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p. 1146 - 1151
(2013/09/24)
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- Design and synthesis of biquinolone-isoniazid hybrids as a new class of antitubercular and antimicrobial agents
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Twenty four biquinolone-isoniazid hybrids were designed based on molecular hybridization technique and synthesized via multicomponent cyclocondensation (MCC) approach. All the newly synthesized compounds were screened for their antimicrobial and antituber
- Jardosh, Hardik H.,Patel, Manish P.
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p. 348 - 359
(2013/10/01)
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- An efficient one-pot synthesis, structure, antimicrobial and antioxidant investigations of some novel quinolyldibenzo[b,e][1,4]diazepinones
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A highly improved one-pot procedure for the synthesis of diazepinones, which incorporate a bioactive quinoline nucleus, under catalyst-, and solvent-free environment has been developed. The method allowed us to achieve the products in high yields without requiring a chromatographic separation. All new quinolyldibenzo[b,e][1,4]diazepinones 6a-h thus obtained were further treated to achieve N10-allylated products 7a-h by a simple allylation. The structure of all new synthesized compounds was established based on elemental analysis, mass, 1H NMR, 13C NMR, IR spectral data, 2D NMR experiments, and single crystal X-ray study. From in vitro antimicrobial activity studies it revealed all are active against Gram positive (Streptococcus pneumoniae, Clostridium tetani, and Bacillus subtilis), Gram negative (Salmonella typhi, Vibrio chlolerae and Escherichia coli), M. Tuberculosis H37RV bacteria, and fungus like Candia albicans and Aspergillus fumigatus. All were also found to display good antioxidant activity of a ferric reducing power.
- Parmar, Narsidas J.,Barad, Hitesh A.,Pansuriya, Bhavesh R.,Teraiya, Shashikant B.,Gupta, Vivek K.,Kant, Rajni
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p. 3816 - 3821
(2012/07/16)
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- Zn(OTf)2-catalyzed three component, one-pot cyclocondensation reaction of some new octahydroquinazolinone derivatives and access their bio-potential
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An efficient synthesis of some new octahydroquinazolinone derivatives 4a-x by the cyclocondensation reaction of corresponding 2-thi(oxo)-1,2- dihydroquinoline-3-carbaldehyde 1a-e, 1,3-dicarbonyl compounds 2a-b, and substituted urea 3a-c using zinc triflat
- Shah, Pushpak M.,Patel, Manish P.
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p. 1188 - 1198
(2012/08/08)
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- Novel 1-alkynyl substituted 1,2-dihydroquinoline derivatives from nimesulide (and their 2-oxo analogues): A new strategy to identify inhibitors of PDE4B
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A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as
- Pal, Sarbani,Durgadas, Shylaprasad,Nallapati, Suresh Babu,Mukkanti, Khagga,Kapavarapu, Ravikumar,Meda, Chandana Lakshmi T.,Meda, Kishore V.L.,Pal, Manojit
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supporting information; scheme or table
p. 6573 - 6576
(2011/12/04)
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- An effective Cu(ii) quenching fluorescence sensor in aqueous solution and 1D chain coordination polymer framework
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In the article, a novel fluorescent probe for the copper cation based on fluorescence quenching mechanism was designed. It exhibited high selectivity for Cu(ii) over other common metal ions in aqueous media. Furthermore the coordination between Cu(ii) and the organic molecule sensor fabricated an interesting 1D chain coordination polymer framework.
- Liu, Zeng-Chen,Yang, Zheng-Yin,Li, Tian-Rong,Wang, Bao-Dui,Li, Yong,Qin, Dong-Dong,Wang, Ming-Fang,Yan, Mi-Hui
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supporting information; scheme or table
p. 9370 - 9373
(2011/11/05)
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