- Design, synthesis, and evaluation of different scaffold derivatives against NS2B-NS3 protease of dengue virus
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The number of deaths or critical health issues is a threat in the infection caused by Dengue virus, which complicates the situation, as only symptomatic treatment is the current solution. In this regard we have targeted the dengue protease NS2B-NS3 that is responsible for the replication. The series was designed with the help of molecular modeling approach using docking protocols. The series comprised of different scaffolds viz. cinnamic acid analogs (CA1–CA11), chalcone (C1–C10) and their molecular hybrids (Lik1–Lik10), analogs of benzimidazole (BZ1-BZ5), mercaptobenzimidazole (BS1-BS4), and phenylsulfanylmethylbenzimidazole (PS1-PS4). Virtual screening of various natural phytoconstituents was employed to determine the interactions of designed analogs with the residues of catalytic triad in the active site of NS2B-NS3. We have further synthesized the selected leads. The synthesized analogs were evaluated for the cytotoxicity and NS2B-NS3 protease inhibition activity and compared with known anti-dengue natural phytoconstituent quercetin as the standard. CA2, BZ1, and BS2 were found to be more potent and efficacious than the standard quercetin as evident from the protease inhibition assay.
- Ganji, Lata R.,Gandhi, Lekha,Musturi, Venkataramana,Kanyalkar, Meena A.
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p. 285 - 301
(2020/11/19)
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- A combined experimental and DFT investigation of mono azo thiobarbituric acid based chalcone disperse dyes
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A number of monoazo dyes were synthesized by the reaction of 4-aminoacetophenone with different substituted benzaldehydes to give a new series of chalcone derivatives. The diazonium salts of these chalcones then allowed to react with thiobarbituric acid to produce the appropriate azo dye. The structures of the newly synthesized dyes were assigned by IR, NMR spectral data. IR study confirmed the existence of azo-dioxothioxo tautomer in the solid phase while 1H NMR study indicated the predominance of azoenol-oxothioxo or hydrazo-dioxothioxo tautomers. The geometries of the azo and hydrazo tautomeric forms and their electronic absorption of the dyes were optimized at B3LYP/6-311G level of theory. All the azo compounds were evaluated for their dyeing performance on polyester fibers, and PET. All the synthesized dyes gave moderate to excellent fastness properties on PET fiber. The effects of the nature of the substituents on the color and dyeing properties of these dyes have been evaluated. The mechanism of dyeing polyester fiber was discussed.
- El-Sadany, Samir K.,El-atawy, Mohamed A.,Hamed, Ezzat A.,Mahmoud, Mona N.,Omar, Alaa Z.
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- Chalcones and their B-aryl analogues as myeloperoxidase inhibitors: In silico, in vitro and ex vivo investigations
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In the present study, a series of chalcones and their B-aryl analogues were prepared and evaluate as inhibitors of myeloperoxidase (MPO) chlorinating activity, using in vitro and ex vivo assays. Among these, B-thiophenyl chalcone (analogue 9) demonstrated inhibition of in vitro and ex vivo MPO chlorinating activity, exhibiting IC50 value of 0.53 and 19.2 μM, respectively. Potent ex vivo MPO inhibitors 5, 8 and 9 were not toxic to human neutrophils at 50 μM, as well as displayed weak 2,2-diphenyl-1-pycrylhydrazyl radical (DPPH?) and hypochlorous acid (HOCl) scavenger abilities. Docking simulations indicated binding mode of MPO inhibitors, evidencing hydrogen bonds between the amino group at 4′position (ring A) of chalcones with Gln91, Asp94, and Hys95 MPO residues. In this regard, the efficacy and low toxicity promoted aminochalcones and arylic analogues to the rank of hit compounds in the search for new non-steroidal anti-inflammatory compounds.
- Santos, Mariana Bastos dos,Carvalho Marques, Beatriz,Miranda Ayusso, Gabriela,Rocha Garcia, Mayara Aparecida,Chiquetto Paracatu, Luana,Pauli, Ivani,Silva Bolzani, Vanderlan,Defini Andricopulo, Adriano,Farias Ximenes, Valdecir,Zeraik, Maria Luiza,Regasini, Luis Octavio
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- Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives
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Novel enamine derivatives were synthesized from the reaction of lactone and chalcones and their antiproliferative and cytotoxic activities against six cancer cell lines (e. g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell lines (e. g., FL) were investigated along with their mode of interactions with CT-DNA. Most of the enamine derivatives with IC50 values of 86–168 μM demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5-fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (~6 nm), indicating that they bind to the DNA by way of an intercalative or minor groove binding mode. The binding constants of the compounds are in the range of 0.1×103 M?1–2.3×104 M?1. The antiproliferative activity of studied enamine derivatives could possibly be due to their DNA binding as well as their cytotoxic properties. In addition to these assays, the chalcones and enamine derivatives were investigated by molecular docking to calculate the synergistic effect of antiproliferative activities against six human cancer cell lines.
- Burcu Gürdere, Meliha,Aydin, Ali,Yencilek, Belk?z,Ertürk, Fatih,?zbek, O?uz,Erkan, Sultan,Budak, Yakup,Ceylan, Mustafa
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- Structure-aided drug development of potential neuraminidase inhibitors against pandemic H1N1 exploring alternate binding mechanism
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Abstract: The rate of mutability of pathogenic H1N1 influenza virus is a threat. The emergence of drug resistance to the current competitive inhibitors of neuraminidase, such as oseltamivir and zanamivir, attributes to a need for an alternative approach. The design and synthesis of new analogues with alternate approach are particularly important to identify the potential neuraminidase inhibitors which may not only have better anti-influenza activity but also can withstand challenge of resistance. Five series of scaffolds, namely aurones (1a–1e), pyrimidine analogues (2a–2b), cinnamic acid analogues (3a–3k), chalcones (4a–4h) and cinnamic acid linkages (5a–5c), were designed based on virtual screening against pandemic H1N1 virus. Molecular modelling studies revealed that the designed analogues occupied 430-loop cavity of neuraminidase. Docking of sialic acid in the active site preoccupied with the docked analogues, i.e. in 430-loop cavity, resulted in displacement of sialic acid from its native pose in the catalytic cavity. The favourable analogues were synthesized and evaluated for the cytotoxicity and cytopathic effect inhibition by pandemic H1N1 virus. All the designed analogues resulting in displacement of sialic acid suggested alternate binding mechanism. Overall results indicated that aurones can be measured best among all as potential neuraminidase inhibitor against pandemic H1N1 virus. Graphical abstract: [Figure not available: see fulltext.].
- Malbari, Khushboo D.,Chintakrindi, Anand S.,Ganji, Lata R.,Gohil, Devanshi J.,Kothari, Sweta T.,Joshi, Mamata V.,Kanyalkar, Meena A.
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p. 927 - 951
(2019/02/07)
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- 1,3,4-oxadiazole/chalcone hybrids: Design, synthesis, and inhibition of leukemia cell growth and EGFR, Src, IL-6 and STAT3 activities
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A new series of 1,3,4-oxadiazole/chalcone hybrids was designed, synthesized, identified with different spectroscopic techniques and biologically evaluated as inhibitors of EGFR, Src, and IL-6. The synthesized compounds showed promising anticancer activity, particularly against leukemia, with 8v being the most potent. The synthesized compounds exhibited strong to moderate cytotoxic activities against K-562, KG-1a, and Jurkat leukemia cell lines in MTT assays. Compound 8v showed the strongest cytotoxic activity with IC50 of 1.95 μM, 2.36 μM and 3.45 μM against K-562, Jurkat and KG-1a leukemia cell lines, respectively. Moreover; the synthesized compounds inhibited EGFR, Src, and IL-6. Compound 8v was most effective at inhibiting EGFR (IC50 = 0.24 μM), Src (IC50 = 0.96 μM), and IL-6 (% of control = 20%). Additionally, most of the compounds decreased STAT3 activation.
- Fathi, Marwa Ali A.,Abd El-Hafeez, Amer Ali,Abdelhamid, Dalia,Abbas, Samar H.,Montano, Monica M.,Abdel-Aziz, Mohamed
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p. 150 - 163
(2018/12/11)
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- EGFR inhibitors and apoptotic inducers: Design, synthesis, anticancer activity and docking studies of novel xanthine derivatives carrying chalcone moiety as hybrid molecules
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One of the helpful ways to improve the effectiveness of anticancer agents and weaken drug resistance is to use hybrid molecules. therefore, the current study intended to introduce 20 novel xanthine/chalcone hybrids 9–28 of promising anticancer activity. Compounds 10, 11, 13, 14, 16, 20 and 23 exhibited potent inhibition of cancer cells growth with IC50 ranging from 1.0 ± 0.1 to 3.5 ± 0.4 μM compared to doxorubicin with IC50 ranging from 0.90 ± 0.62 to 1.41 ± 0.58 μM and that compounds 11 and 16 were the best. To verify the mechanism of their anticancer activity, compounds 10, 11, 13, 14, 16, 20 and 23 were evaluated for their EGFR inhibitory effect. The study results revealed that compound 11 showed IC50 = 0.3 μM on the target enzyme which is more potent than staurosporine reference drug (IC50 = 0.4 μM). Accordingly, the apoptotic effect of the most potent compounds 11 was extensively investigated and showed a marked increase in Bax level up to 29 folds, and down-regulation in Bcl2 to 0.28 fold, in comparison to the control. Furthermore, the effect of compound 11 on Caspases 3 and 8 was evaluated and was found to increase their levels by 8 and 14 folds, respectively. Also, the effect of compound 11 on the cell cycle and its cytotoxic effect were examined. Moreover, a molecular docking study was adopted to confirm mechanism of action.
- Abou-Zied, Hesham A.,Youssif, Bahaa G.M.,Mohamed, Mamdouh F.A.,Hayallah, Alaa M.,Abdel-Aziz, Mohamed
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- Gold nanodots self-assembled polyelectrolyte film as reusable catalyst for reduction of nitroaromatics
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Separation of homogeneous catalyst from the reaction mixture is a crucial and difficult process in any catalytic process. To address this issue, a new class of multifunctional catalyst in the form of film was developed using a facile approach to enjoy the advantages of homogeneous catalyst with the versatility of heterogeneous catalyst. To achieve the same, methionine-capped gold nanodots (AuNDs) were self-assembled on a cationic polyelectrolyte modified glass plate for the catalytic reduction of nitro functional groups in the presence of olefinic double bond at mild conditions. Separation of this reusable catalytic film from the reaction mixture is very simple and advantageous when compared to the currently available and conventional catalytic systems. Kinetics of nitro reduction was monitored using absorption spectroscopy and the product formation was confirmed by 1H and 13CNMR analyses. Prepared AuNDs catalyst was characterized using UV-Vis spectroscopy, X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), high-resolution transmission electron microscopy (HRTEM), cyclic voltammetry and atomic force microscopy (AFM) techniques. Graphical Abstract: SYNOPSIS?Colloidal gold nanoparticles are efficient catalysts for organic reactions. But the removal of homogeneous gold colloids from the reaction mixture is very difficult. To address this issue, gold nanodots were synthesized and self-assembled over polyelectrolyte film to form catalytic plates. Removal of these reusable catalytic plates from the reaction mixture is facile.[Figure not available: see fulltext.].
- Viswanathan, Perumal,Ramaraj, Ramasamy
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- New 1,2,4-triazole-Chalcone hybrids induce Caspase-3 dependent apoptosis in A549 human lung adenocarcinoma cells
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A series of novel 1, 2, 4-triazole/chalcone hybrids was prepared and identified with different spectroscopic techniques. The prepared compounds showed remarkable cytotoxic activity against different cancer cell lines. Compounds 24, 25, 27, 41 and 47 had shown the highest cytotoxicity among the tested compounds against human lung adenocarcinoma A549 cells with IC50 ranging from 4.4 to 16.04 μM compared to cisplatin with IC50 of 15.3 μM. Flow cytometric analysis of the tested compounds showed an increase in the number of apoptotic cells in a dose-dependent manner. The further mechanistic study demonstrated that 1, 2, 4-triazole-chalcone hybrids induced apoptosis via increased level of proapoptotic protein Bax, release of cytochrome c from mitochondria and activation of caspase-3/8/9 proteins. However, general caspase inhibition by the pan-caspase inhibitor, z-VAD-fmk, significantly decreased the apoptosis induced by the tested hybrids, suggesting dependency of apoptosis on activation of the caspase-3 pathway.
- Ahmed, Fatma F.,Abd El-Hafeez, Amer Ali,Abbas, Samar H.,Abdelhamid, Dalia,Abdel-Aziz, Mohamed
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p. 705 - 722
(2018/04/17)
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- 3-Aminomethyl pyridine chalcone derivatives: Design, synthesis, DNA binding and cytotoxic studies
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Herein we report design, synthesis, and anticancer activity of compounds 6a–h and 11a–j. Compounds 6a–f were designed based on 3-aminomethyl pyridine attached to different acetamide derivatives and in compounds 6g–h it was attached to coumarin moiety. Coumarin containing compounds 6g–h showed very poor anticancer activity against both A549 (Lungs cancer cell line), and MCF-7 (Breast cancer cell line) cell lines in MTT assay. Compounds 11a–j were designed as derivatives of 3-aminomethyl pyridine and 4-amino chalcones. A series of chalcone derivatives of 3-aminomethyl pyridine 11a–j have been synthesized and screened for their in vitro anticancer activity and DNA binding affinity. Most of the compounds showed very good antimitotic activity against A549 cell line as compared to fluorouracil. Compounds 11g and 11i were selected for DNA-binding studies as they showed excellent activity against cancer cell lines in MTT assay. CT-DNA binding affinity of compounds 11g and 11i have been investigated by UV based DNA titration and fluorescence emission study against DNA-EtBr complex. Interestingly, compound 11i has displayed excellent antiproliferative activity, with IC50 0.0067?±?0.0002?μm, against MCF-7 cell line. Compound 11i has been studied for its cytotoxicity using MTT, LDH, as well as EtBr/AO assay and was found to induce apoptosis in the cancerous cell line.
- Durgapal, Sunil Dutt,Soni, Rina,Umar, Shweta,Suresh, Balakrishnan,Soman, Shubhangi S.
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p. 1279 - 1287
(2018/06/29)
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- Design, Synthesis, and Antiviral Activity of Novel Chalcone Derivatives Containing a Purine Moiety
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To find new antiviral agents, novel chalcone derivatives containing a purine moiety were designed and synthesized by combining bioactive substructures. The antiviral activities of the derivatives against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) were evaluated. Results showed that most of the derivatives showed antiviral activities. Compounds 3n and 3p exhibited excellent curative, protective and inactivation activities against TMV, with the EC50 values of 452.4, 416.2, 241.2 and 438.7, 418.6, 261.7 μg?mL?1, respectively, which were better than those of ribavirin (585.8, 436.0 and 268.7 μg?mL?1). Compounds 3n and 3p showed remarkable curative and protective activities against CMV. Compound 3n showed a moderate affinity to TMV coat protein, with binding constant Ka and Kd values of 1.5 × 104 L?mol?1 and 79.8 μmol?L?1, respectively. These findings provided an important structural insight for further designs of highly active chalcone derivatives and a basis for further study on their mechanism of action.
- Gan, Xiuhai,Wang, Yanjiao,Hu, Deyu,Song, Baoan
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p. 665 - 672
(2017/05/29)
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- Synthesis and biological evaluation of some new pyrazoline derivatives as anti-inflammatory agents
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A series of pyrazolyl urea 3a-l and pyrazolyl sulphonamide 4a-l derivatives have been synthesized by the reaction of respective pyrazoline derivatives 2a-l with phenylisocyanate and p-acetamidobenzenesulphonylchloride respectively. All the synthesized compounds are characterized by IR, 1H NMR, mass spectral data, and elemental analysis. The compounds have been screened for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation potential.
- Amir, Mohd,Ali, Sazid,Somakala
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p. 478 - 485
(2017/01/18)
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- Naphthoquinone-based chalcone hybrids and derivatives: Synthesis and potent activity against cancer cell lines
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Novel naphthoquinone-based chalcones were prepared from the reaction between 3-bromo-nor-β-lapachone and amino-chalcones. Lapachone derivatives are also described here. All the substances were evaluated against cancer and normal cell lines and several compounds demonstrated potent antitumor activity. This journal is
- Jardim, Guilherme A. M.,Guimares, Tiago T.,Pinto, Maria Do Carmo F.R.,Cavalcanti, Bruno C.,De Farias, Kaio M.,Pessoa, Claudia,Gatto, Claudia C.,Nair, Divya K.,Namboothiri, Irishi N. N.,Da Silva Jnior, Eufrnio N.
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p. 120 - 150
(2015/02/02)
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- On the investigation of hybrid quinones: Synthesis, electrochemical studies and evaluation of trypanocidal activity
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In our continued search for novel trypanocidal compounds, arylamine, chalcone, triazolic, triazole-carbohydrate and chalcogenium derivatives containing a naphthoquinone scaffold were prepared; in addition to electrochemical studies, these compounds were evaluated against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease. Among the thirty-eight compounds herein evaluated, six were found to be more potent against trypomastigotes than the standard drug benznidazole, with IC50/24 h values between 52.9 and 89.5 μM.
- Jardim, Guilherme A. M.,Reis, Wallace J.,Ribeiro, Matheus F.,Ottoni, Flaviano M.,Alves, Ricardo J.,Silva, Thaissa L.,Goulart, Marilia O. F.,Braga, Antonio L.,Menna-Barreto, Rubem F. S.,Salom?o, Kelly,De Castro, Solange L.,Da Silva Júnior, Eufranio N.
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p. 78047 - 78060
(2015/09/28)
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- Dual inhibition of the α-glucosidase and butyrylcholinesterase studied by Molecular Field Topology Analysis
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A striking dual inhibition of enzymes α-glucosidase and butyrylcholinesterase by small drug-like molecules, including 1,4-disubstituted-1,2,3-triazoles, chalcones, and benzothiazepines, was rationalized with the help of Molecular Field Topology Analysis, a 3D QSAR technique similar to CoMFA. A common pharmacophore supported the concept of a link existing between type-2 diabetes mellitus and Alzheimer's disease. These findings will be instrumental for rational design of drug candidates for both of these conditions.
- Jabeen, Farukh,Oliferenko, Polina V.,Oliferenko, Alexander A.,Pillai, Girinath G.,Ansari, Farzana Latif,Hall, C. Dennis,Katritzky, Alan R.
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p. 228 - 242
(2014/05/20)
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- Synthesis of amino chalcones in presence of ionic liquid as soluble support
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A microwave-assisted liquid phase synthesis of aminochalcones was developed by using aldehyde-functionalized ionic liquid as soluble support. Ionic liquid bound aminoacetophenone was treated with aromatic aldehyde to give supported chalcone derivatives. After cleavage, the target compounds were obtained in 83-92 % yields and ≥ 95 % purities without column chromatographic purification. The recovered aldehyde-functionalized ionic liquid could be reused for several times without affecting its activity and the yields of desired compounds were between 86-89 %. These results indicated that the presented method could be applied efficiently to the liquid phase combinatorial chemistry based on aldol condensation.
- Pan, Xianhua,Yi, Fengping,Zhang, Xuan,Chen, Shihong
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p. 3809 - 3813
(2012/09/07)
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- Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids
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A group of novel nitric oxide (NO) donating chalcone derivatives was prepared by binding various amino chalcones with different NO donating moieties including; nitrate ester, oximes and furoxans. Most of the prepared compounds showed significant anti-inflammatory activity using carrageenan-induced rat paw edema method compared with indomethacin. The prepared compounds exhibited more protection than indomethacin in regard to gastric toxicity. Histopathological investigation confirmed the beneficial effects of the NO releasing compounds in reducing ulcer formation. The incorporation of the NO-donating group into the parent chalcone derivatives caused a moderate increase in the anti-inflammatory activity with a marked decrease in gastric ulcerations compared to their parent chalcone derivatives.
- Abuo-Rahma, Gamal El-Din A.A.,Abdel-Aziz, Mohamed,Mourad, Mai A.E.,Farag, Hassan H.
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experimental part
p. 195 - 206
(2012/02/06)
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- A study of anti-inflammatory and analgesic activity of new 2,4,6-trisubstituted pyrimidines
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Chalcone derivatives (3a - m) were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes according to Claisen-Schmidt condensation. These chalcones, on reaction with guanidine hydrochloride under basic alcoholic conditions gave 2,4,6-trisubstituted pyrimidines (5a - m) in quantitative yields. All the newly synthesized pyrimidines were characterized by means of IR, 1H- and 13CNMR, Electron Ionization (EI)-mass and elemental analyses and screened for anti-inflammatory and analgesic activities by in vivo. 2-Amino-4-(4-aminophenyl)-6-(2,4-dichlorophenyl)pyrimidine (5b) and 2-amino-4-(4-aminophenyl)- 6-(3-bromophenyl) pyrimidine (5d) were found to be the most potent anti-inflammatory and analgesic activity compared with ibuprofen, reference standard. And also it was found that compound 5b identified as lead structure among all in both the activities. Pyrimidines which showed good anti-inflammatory activity also displayed better analgesic activity.
- Yejella, Rajendra Prasad,Atla, Srinivasa Rao
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scheme or table
p. 1079 - 1082
(2011/10/05)
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- Synthesis and antimicrobial activity of some new 2,4,6-trisubstituted pyrimidines
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Chalcone derivatives [3(a-m)] were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes in dilute ethanolic potassium hydroxide solution at room temperature according to Claisen-Schmidt condensation. These chalcones react with guanidine hydrochloride in a basic alcoholic media to give 2,4,6-trisubstituted pyrimidines [5(a-m)]. All these pyrimidines were characterized by means of their IR, 1H NMR and elemental analyses and screened for their antimicrobial activity. Some of these compounds showed significant antimicrobial activity.
- Prasad, Y. Rajendra,Rao, B. Bhaskar,Agarwal,Rao, A. Srinivasa
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scheme or table
p. 641 - 644
(2011/12/15)
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- Synthesis and analgesic activity of some chalcones
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A series of novel 1-(4′-aminophenyl)-3-(substituted aryl/heteroaryl)-2-propen-1-ones (1-16) have been synthesized by treating 4-amino acetophenone with various substituted aromatic and unsubstituted heterocyclic aldehydes in presence of methanol and aqueous alkaline solution at room temperature. Their structures were confirmed by IR, 1H NMR, 13C NMR, EI-MS spectra and elemental analyses data. The synthesized compounds were investigated for their analgesic activity. Compounds 6 and 15 exhibited maximum analgesic activity. Chalcones with electron releasing substituent like amino, hydroxyl, methyl, halogens etc exhibited good analgesic activity.
- Srinivasa Rao
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experimental part
p. 4373 - 4376
(2012/02/14)
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- Synthesis of new chalcone derivatives containing acridinyl moiety with potential antimalarial activity
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A series of novel chalcones bearing acridine moiety attached to the amino group in their ring A have been synthesized through noncatalyzed nucleophilic aromatic substitution reaction between various 3′-aminochalcone or 4′-aminochalcones and 9-chloroacridine. The synthesized chalcone derivatives have been characterized and screened for in vitro antimalarial activity against Plasmodium falciparum NF-54. All the chalcones showed complete inhibition at concentration of 10 μg/mL and above while three compounds showed significant inhibition at concentration of 2 μg/mL. The three most active chalcone derivatives were screened for in vivo activity as well, but no significant inhibition in parasitaemia was observed when given intraperitoneally to Plasmodium yoelii infected mice model.
- Tomar,Bhattacharjee,Kamaluddin,Rajakumar,Srivastava, Kumkum,Puri
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scheme or table
p. 745 - 751
(2010/04/04)
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- The synthesis and structure-activity relationship of substituted N-phenyl anthranilic acid analogs as amyloid aggregation inhibitors
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It is believed that β-amyloid aggregation is an important event in the development of Alzheimer's disease. In the course of our studies to identify β-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for β-amyloid inhibition activity. The synthesis, structure-activity relationship, and in vivo activity of these analogs are discussed.
- Simons, Lloyd J.,Caprathe, Bradley W.,Callahan, Michael,Graham, James M.,Kimura, Takenori,Lai, Yingjie,LeVine III, Harry,Lipinski, William,Sakkab, Annette T.,Tasaki, Yoshikazu,Walker, Lary C.,Yasunaga, Tomoyuki,Ye, Yuyang,Zhuang, Nian,Augelli-Szafran, Corinne E.
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scheme or table
p. 654 - 657
(2009/09/06)
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- Synthesis of some new pyrazolines from 4-amino-4-methoxybenzalace-tophenone as dyestuffs intermediates
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New aminopyrazoline derivatives (II-V) has been obtained by the reaction of new benzalacetophenone derivatives (1a, b) with hydrazine hydrate and their derivatives. Further reactions were carried out on pyrazolines (VI-XI). The structural determination of the prepared compounds has been confirmed using elemental analysis, chemical reactions and spectral data.
- Sayed,Eman,Selim
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- Kinetic Study of the Homolytic Brominolysis of 1,2-Diarylcyclopropanes
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The rate constants for the photolytic brominolysis of 22 trans-1,2-diarylcyclopropanes in carbon disulfide relative to an internal standard, p-chlorotoluene, have been determined.The products of the brominolysis are 1,3-dibromo-1,3-diarylpropanes.The rate constants range over 5 orders of magnitude, being enhanced by electrondonating substituents on one or both benzene rings.The quantitative size of the substituent effect (ρ) at either involved carbon center is a function of the substituent at the other center.This fact suggests a continuum of transition-state structures with varying degrees of bond breaking and charge separation.
- Applequist, Douglas E.,Gdanski, Rick D.
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p. 2502 - 2510
(2007/10/02)
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