- Novel thienopyrimidine-aminothiazole hybrids: Design, synthesis, antimicrobial screening, anticancer activity, effects on cell cycle profile, caspase-3 mediated apoptosis and VEGFR-2 inhibition
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A series of novel hybrid compounds of hexahydrobenzo[4,5]thieno[2,3-d]pyrimidine with aminothiazole scaffolds were synthesized. The synthesized compounds were evaluated for their cytotoxic activity against the NCI-60 human tumor cell line panel. Compounds 7c, 7d and 7e exhibited significant antiproliferative activities at 10?5 M dose. Compound 7c exhibited excellent cytotoxic activity against CNS cancer cell lines including SNB-75 and SF-295 as well as renal cancer cell line CAKI-1 when compared with sorafenib as standard anticancer drug. In addition, compound 7d showed almost comparable anticancer activity to sorafenib against SNB-75 cell line and displayed moderate activity against SF-295 and CAKI-1 cell lines in comparison to sorafenib. Compound 7c inhibited the vascular endothelial growth factor receptor 2 (VEGFR-2) with IC50 of 62.48 ± 3.7 nM and decreased both total VEGFR-2 and phosphorylated VEGFR-2 in treated SNB-75 cells suggesting its ability to down regulate cell proliferation, growth, and survival. The flow cytometric analysis showed that 7c displayed its cytotoxic activity through the reduction of the cellular proliferation and induction of cell cycle arrest at the G2/M phase. Compound 7c clearly boosted the level of the apoptotic caspase-3. All the synthesized compounds were also screened for their antibacterial and antifungal activity against four pathogenic strains of both Gram-positive and Gram-negative as well as Candida albicans. Only compound 7d exhibited antifungal activity against Candida albicans compared to nystatin as the standard antifungal compound.
- El-Dash, Yara,Elzayat, Emad,Abdou, Amr M.,Hassan, Rasha A.
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- Design and synthesis of phenoxymethybenzoimidazole incorporating different aryl thiazole-triazole acetamide derivatives as α-glycosidase inhibitors
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A novel series of phenoxymethybenzoimidazole derivatives (9a-n) were rationally designed, synthesized, and evaluated for their α-glycosidase inhibitory activity. All tested compounds displayed promising α-glycosidase inhibitory potential with IC50 values in the range of 6.31 to 49.89?μM compared to standard drug acarbose (IC50 = 750.0 ± 10.0?μM). Enzyme kinetic studies on 9c, 9g, and 9m as the most potent compounds revealed that these compounds were uncompetitive inhibitors into α-glycosidase. Docking studies confirmed the important role of benzoimidazole and triazole rings of the synthesized compounds to fit properly into the α-glycosidase active site. This study showed that this scaffold can be considered as a highly potent α-glycosidase inhibitor.
- Alamir, Amir,Asgari, Mohammad Sadegh,Bandarian, Fatemeh,Faramarzi, Mohammad Ali,Hajimiri, Mir Hamed,Hamedifar, Haleh,Hosseini, Samanesadat,Iraji, Aida,Larijani, Bagher,Mahdavi, Mohammad,Mojtabavi, Somayeh,Moradi, Shahram,Nasli Esfahani, Anita,Nasli-Esfahani, Ensieh
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- Synthesis of New Binary Thiazole-Based Heterocycles and Their Molecular Docking Study as COVID-19 Main Protease (Mpro) Inhibitors
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Abstract: Isolated polynuclear binary heterocyclic compounds containing thiazole building block combined with benzofuran, pyrrole, thiazole, or thiophene via carboxamide and/or secondary amine as a junction are presented. The synthetic strategy of those is based on utilization of 2-chloroacetamido-4-phenylthiazole in the synthesis of binary heterocyclic compounds by cyclocondensation with salicylic aldehyde, acetonitrile derivatives, ammonium thiocyanate, 3-mercaptoacrylonitrile derivatives, and/or 3-mercaptoacrylate derivatives. The prepared binary thiazole-based heterocycles have been studied as protease (Mpro) inhibitors by molecular docking for visualization of their orientation and interactions with COVID-19 units using hydroxychloroquine as a reference molecule.
- Abdel-Latif, E.,Fekri, A.,Khalifa, M. E.,Khatab, T. K.
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p. 1767 - 1773
(2021/11/01)
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- Synthesis, biological evaluation, and docking studies of novel 5,6-diaryl-1,2,4-triazine thiazole derivatives as a new class of α-glucosidase inhibitors
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A novel 5,6-diaryl-1,2,4-triazine thiazole derivatives (7a-7q) were synthesized and characterized by 1H NMR and 13C NMR and evaluated for their α-glucosidase inhibitory activity. All tested compounds displayed good α-glucosidase inhibitory activity with IC50 values ranging between 2.85 ± 0.13 and 14.19 ± 0.23 μM when compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μM). Compound 7i (IC50 = 2.85 ± 0.13 μM) exhibited the highest activity among this series of compounds. Molecular docking studies were carried out in order to investigate the binding mode of this class of compounds to α-glucosidase. This study showed that these 5,6-diaryl-1,2,4-triazine thiazole derivatives are a new class of α-glucosidase inhibitors.
- Wang, Guangcheng,Peng, Zhiyun,Gong, Zipeng,Li, Yongjun
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p. 195 - 200
(2018/04/02)
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- Β - secretase enzyme has the function of inhibiting compound, the preparation of the compounds and use thereof
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The invention discloses a compound capable of inhibiting beta-secretase, and a preparation method and application thereof. The structure of the compound is shown in a formula I, formula II or formula III as described in the specification. In the formula I, X is S or NH; R1 is selected from hydrogen and nitro group; R2 and R4 are same or different and independently selected from the group consisting of hydrogen, halogen, nitro group and substituted aryl group; R3 is selected from the group consisting of hydrogen, nitro group, straight-chain and branched-chain alkyl and substituted alkyl groups with a carbon number of 1 to 4, alkylamino or alkyloxy group with a carbon number of 1 to 4 and alkylamido group with a carbon number of 1 to 4; R is located at position 2, 3 or 4 of a benzene ring and selected from the group consisting of hydrogen, straight-chain and branched-chain alkyl and substituted alkyl groups with a carbon number of 1 to 4, alkylamino or alkyloxy group with a carbon number of 1 to 4 and alkylamido group with a carbon number of 1 to 4. In the formula II, R is selected from different substituted aryl groups. In the formula III, R is selected from hydrogen or cyano group. Experiments prove that the compound provided by the invention has good beta-secretase inhibitory activity and has wide application values as a beta-secretase inhibitor.
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- Synthesis and biological screening of diethyl [N-(thiazol-2-yl)carbamoyl]methylphosphonates
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A three-step synthesis, involving condensation of bromomethyl aryl ketones with urea to afford 2- aminothiazoles, their chloroacetylation and subsequent solvent-free Arbuzov phosphonation has afforded a series of novel diethyl [N-(thiazol-2-yl)carbamoyl]methylphosphonates 3a-3f in good overall yields; the 4- carboxythiazole analogue 3g was obtained by selective hydrolysis of the corresponding ethyl ester 3f. The phosphonate esters exhibited significant anti-cancer activity (nM - low μM IC50 values) against SH-SY5Y cells and, in one case, 7.6 μM MIC90 anti-TB activity against the virulent M. tuberculosis H37Rv strain; the chloroacetamido precursors all exhibited some antimalarial (PfLDH) activity, three with IC50 values in the range 1.0 - 8.9 μM.
- Olawode, Emmanuel O.,Tandlich, Roman,Prinsloo, Earl,Isaacs, Michelle,Hoppe, Heinrich,Seldon, Ronnett,Warner, Digby F.,Steenkamp, Vanessa,Kaye, Perry T.
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p. 110 - 118
(2018/10/26)
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- Synthesis, characterization and drug-likeness predictions of 1,3-thiazole and benzothiazole derivatives
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Heterocyclic compounds bearing nitrogen and sulphur in the main skeleton are reported to be a bioactive group. Thiazole and benzothiazole moieties are biologically significant class of this group. This research focus on the synthesis and characterization of 1,3-thiazole and benzothiazole derivatives. Drug likeness predictions were also undertaken for these newly synthesized compounds.
- Naqvi, Arshi
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p. 3134 - 3139
(2019/01/05)
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- 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and?docking studies
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In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog 41 (IC50 = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization.
- Yan, Gang,Hao, Lina,Niu, Yan,Huang, Wenjie,Wang, Wei,Xu, Fengrong,Liang, Lei,Wang, Chao,Jin, Hongwei,Xu, Ping
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p. 462 - 475
(2017/06/19)
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- Design and discovery of novel thiazole derivatives as potential MMP inhibitors to protect against acute lung injury in sepsis rats: Via attenuation of inflammation and apoptotic oxidative stress
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Acute lung injury (ALI) is considered to be an inflammatory syndrome of the airway system that is initiated by failure of the respiratory system. In this study, we evaluated the possible benefits of some novel thiazole derivatives against ALI. These derivatives were synthesised and evaluated for the inhibition of MMP-8 and MMP-2. Most of the tested compounds had better inhibitory activity for MMP-8 than for MMP-2, with compound 26 being the most potent analogue among the tested series. Thus, compound 26 was further investigated to determine its beneficial effects in an ALI model of rats with sepsis. In vivo results suggested that compound 26 significantly reduced the protein concentration together with a decline in enhanced leukocytes compared with those in ALI induced by cecal ligation and puncture. The effect of compound 26 on myeloperoxidase activity was also quantified, which was found to be significantly reduced at the maximum tested dose of 20 mg kg-1. The protective effect of compound 26 against ALI was also established to occur via the significant modulation of various biomarkers; for example, the malondialdehyde level was found to be reduced, while there were increased levels of superoxide dismutase and glutathione. Thus, it is proposed that compound 26 exerts a protective effect against ALI via modulation of the antioxidant status. Furthermore, the compounds tested caused significant attenuation of the levels of tumour necrosis factor-α, interleukin-1β, and interleukin-6, and protected the lung through the modulation of systemic inflammatory mediators in septic rats. In conclusion, we identified a novel series of thiazoles, which potentially exert protective effects against ALI via the inhibition of numerous pathways.
- Ge, Lingqing,Hu, Qiaozhen,Shi, Mengrao,Yang, Huiyun,Zhu, Guoji
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p. 32909 - 32922
(2017/07/10)
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- Synthesis, antibacterial, antifungal, and antioxidant evaluation of some new thiazole clubbed oxadiazole derivatives
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A series of thiazole incorporated oxadiazole derivatives (6a-6f) was synthesized by reacting 2-chloro-N-(4-(4-substituted phenyl) thiazol-2-yl) acetamide with 5-pyridine-1,3,4-oxadiazole-2-thione using multistep solution phase chemistry. The synthesized compounds were structurally characterized on the basis of elemental analysis and using various spectral data. All the compounds were evaluated for their in vitro antibacterial, antifungal, and antioxidant activity. Some of the new compounds exhibited good antimicrobial and antioxidant activity and are suitable candidates for further scientific explorations.
- Monga, Vikramdeep,Singh, Hargyan,Singh, Gurpreet
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- Synthesis and free radical scavenging activity of 2-alkyl/arylchalcogenyl-N-(4-aryl-1,3-thiazol-2-yl)acetamide compounds
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The synthesis of a new series of organochalcogen-derivatives, 2-alkyl/arylchalcogenyl-N-(4-aryl-1,3-thiazol-2-yl)acetamides 5a-r, provided products in satisfactory yields, which varied from 42% to 95%. All these novel compounds were screened for their in vitro free radical scavenging activity against 2,2-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals. Compounds 5 (m, h, i, f, q, g, l, c, n) were effective scavengers against the ABTS radical species but less effective on scavenging the DPPH radical, indicating that the antioxidant effect of these compounds were related to protonated radical scavenger activity.
- Wolf, Lucas,Quoos, Natália,Mayer, Jo?o C.P.,De Souza, Diego,Sauer, André C.,Meichtry, Luana,Bortolotto, Vandreza,Prigol, Marina,Rodrigues, Oscar E.D.,Dornelles, Luciano
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p. 1031 - 1034
(2016/02/16)
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- Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's
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A novel series of thiazole acetamides was synthesized in excellent yields and characterized with the aid of various spectroscopic and elemental analysis. These compounds were evaluated for in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities for possible benefit in Alzheimers disease (AD). Among the synthesized compound, 6d was identified as the most potent compound of AChE (IC50= 3.14 ± 0.16 μM) with a selectivity index (SI) of 2.94 against BuChE. These compounds were further tested for inhibition of Aβ aggregation and β-secretase, where it showed potent inhibition which confirmed its multifactorial benefits in AD. The toxicity and docking study were also carried out to exemplify the pharmacological profile of compound 6d as prospective lead molecule against AD.
- Sun, Zhi-Qing,Tu, Li-Xiang,Zhuo, Feng-Juan,Liu, Song-Xia
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p. 747 - 750
(2016/05/24)
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- 1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation
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In our endeavor towards the development of effective VEGFR-2 inhibitors, three novel series of phthalazine derivatives based on 1-piperazinyl-4-arylphthalazine scaffold were synthesized. All the newly prepared phthalazines 16a-k, 18a-e and 21a-g were evaluated in vitro for their inhibitory activity against VEGFR-2. In particular, compounds 16k and 21d potently inhibited VEGFR-2 at sub-micromolar IC50 values 0.35 ± 0.03 and 0.40 ± 0.04 μM, respectively. Moreover, seventeen selected compounds 16c-e, 16g, 16h, 16j, 16k, 18c-e and 21a-g were evaluated for their in vitro anticancer activity according to US-NCI protocol, where compounds 16k and 21d proved to be the most potent anticancer agents. While, compound 16k exhibited potent broad spectrum anticancer activity with full panel GI50 (MG-MID) value of 3.62 μM, compound 21d showed high selectivity toward leukemia and prostate cancer subpanels [subpanel GI50 (MG-MID) 3.51 and 5.15 μM, respectively]. Molecular docking of compounds16k and 21d into VEGFR-2 active site was performed to explore their potential binding mode.
- Abou-Seri, Sahar M.,Eldehna, Wagdy M.,Ali, Mamdouh M.,Abou El Ella, Dalal A.
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p. 165 - 179
(2015/11/25)
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- Synthesis and biological evaluation of new benzimidazole-thiazolidinedione hybrids as potential cytotoxic and apoptosis inducing agents
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A series of new benzimidazole-thiazolidinedione hybrids has been synthesized and evaluated for their cytotoxic potential against a selected human cancer cell lines of prostate (PC-3 and DU-145), breast (MDA-MB-231), lung (A549) and a normal breast epithelial cells (MCF10A). Among the tested compounds, 11p exhibited promising cytotoxicity with IC50value of 11.46?±?1.46?μM on A549 lung cancer cell line and did not show significant toxicity on normal MCF10A cells. Lung cancer cells (A549) have been used to know the mechanism of cell growth inhibition and apoptosis inducing effect with compound 11p. The treatment of A549?cells with 11p showed typical apoptotic morphology like cell shrinkage, chromatin condensation and horseshoe shaped nuclei formation. Flow-cytometry analysis revealed the G2/M phase of cell cycle arrest in a dose dependent manner. Preliminary mechanistic studies suggested that the cell migration was inhibited through the disruption of F-actin protein. Acridine orange-ethidium bromide (AO-EB), DAPI, annexin V-FITC/propidium iodide, rhodamine-123 and MitoSOX assays suggested the induction of apoptosis in A549 cells by compound 11p.
- Sharma, Pankaj,Srinivasa Reddy,Thummuri, Dinesh,Senwar, Kishna Ram,Praveen Kumar, Niggula,Naidu,Bhargava, Suresh K.,Shankaraiah, Nagula
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supporting information
p. 608 - 621
(2016/09/14)
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- Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE)
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Presently available medications for treatment of organiphosphorus poisoning are not sufficiently effective due to various pharmacological and toxicological reasons. In this regard, herein we report the synthesis of a series of N-thiazolylacetamide monoquaternary pyridinium oximes and its analogs (1a-1b to 6a-6b) with diversely substituted thiazole ring and evaluation of their in vitro reactivation efficacies against nerve agent (sarin, O-ethylsarin and VX) inhibited human erythrocyte acetylcholinesterase (hAChE). Reactivation kinetics was performed to determine dissociation constant (KD), reactivity rate constant (kr) and the second order rate constant (kr2) for all the compounds and compared their efficacies with commercial antidotes viz. 2-PAM and obidoxime. All the newly synthesized oximes were evaluated for their physicochemical parameters (pKa) and correlated with their respective reactivation efficacies to assess the capability of the oxime reactivator. Three of these novel compounds showed promising reactivation efficacies toward OP inhibited hAChE. Molecular docking studies were performed in order to correlate the reactivation efficacies with their interactions in the active site of the AChE.
- Valiveti, Aditya Kapil,Bhalerao, Uma M.,Acharya, Jyotiranjan,Karade, Hitendra N.,Acharya, Badri Narayan,Raviraju,Halve, Anand K.,Kaushik, Mahabir Parshad
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p. 4899 - 4910
(2015/08/03)
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- 2-AMINOTHIAZOLE DERIVATIVE, PREPARATION METHOD, AND USE
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The present invention relates to the preparation of a 2-aminothiazole derivative having a structure as formula (I) and a therapeutic effect thereof for Alzheimer's disease (AD), and a therapeutic effect thereof against transplant rejection, autoimmune diseases, ischemia-reperfusion injury, chronic inflammation response, endotoxemia, and other diseases.
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- 2-AMINOTHIAZOLE DERIVATIVES AND METHODS OF PREPARING AND USING THE SAME
-
2-aminothiazole derivatives represented by formula (I), where R1 and R2 represent cycloalkyls, respectively; or R1 represents a substituted aromatic group, and R2 represents H, a C1-C11 alkyl, —CH2Ph (benzyl), or a methyl ether including a C1-C11 alkyl. R3 is a substituent including an amino group. X represents a carbonyl or a methylene and n is an integer from 0 to 5.
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- 5-Nitro-heteroarylidene analogs of 2-thiazolylimino-4-thiazolidinones as a novel series of antibacterial agents
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In the pursuit of novel antibacterial agents with the 2-thiazolylimino-4- thiazolidinone as a core structure, a series of 5-nitro-heteroarylidene and 5-(2-oxoindolin-3-ylidene) analogs of 2-thiazolylimino-5-arylidene-4- thiazolidinone were synthesized and their antibacterial activities were evaluated against some strains of Gram-positive and Gram-negative bacteria, as well as Helicobacter pylori strains. Biological data indicated that 5-nitrofuran analog 5a and 5-nitroimidazole analog 7a containing no substitutions on the thiazole ring were the most potent compounds.
- Hosseinzadeh, Nouraddin,Hasani, Mohammad,Foroumadi, Alireza,Nadri, Hamid,Emami, Saeed,Samadi, Nasrin,Faramarzi, Mohammad Ali,Saniee, Parastoo,Siavoshi, Farideh,Abadian, Neda,Mahmoudjanlou, Yasaman,Sakhteman, Amirhossein,Moradi, Alireza,Shafiee, Abbas
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p. 2293 - 2302
(2013/07/26)
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- QUINAZOLINONE ANALOGS AND USE OF QUINAZOLINONE ANALOGS FOR TREATING OR PREVENTING CERTAIN VIRAL INFECTIONS
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Provided is a process for treating or preventing a viral infection in a subject, wherein the viral infection is from a flavivirus selected from the group consisting of Hepatitis C Virus (genotypes 1-7) and Japanese Encephalitis Virus. The process includes administering to the subject a therapeutically effective amount of at least one compound represented by the formula:(Formula (I))
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Page/Page column 21
(2013/03/26)
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- Efficient synthesis of new functionalized 2-(hetaryl)thiazoles
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An efficient synthesis of the hitherto unknown ring system, 2-heteroaryl-thiazoles, is described via the reaction of 3-oxo-N-(4- phenylthiazol-2-yl)butanamide (1) with diazotized heterocyclic amine, phenyl isothiocyanate, dimethylformamide-dimethylacetal,
- Bondock, Samir,El-Azab, Hossam,Kandeel, Ez-Eldin M.,Metwally, Mohamed A.
-
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- Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2- ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents
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As a part of our ongoing studies in developing new derivatives as dual antimicrobial/anti-inflammatory agents we describe the synthesis of novel 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones. All newly synthesized compounds were tested for
- Apostolidis,Liaras,Geronikaki,Hadjipavlou-Litina,Gavalas,Sokovic,Glamoclija,Ciric
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p. 532 - 539
(2013/03/13)
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- Synthesis and antioxidant activities of acetamidomethylsulfonyl bis heterocycles-oxazolyl/thiazolyl/imidazolyl-1,3,4-Oxadiazoles
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A new class of acetamidomethylsulfonyl bis heterocycles-oxazolyl-1,3,4- oxadiazoles, -thiazolyl-1,3,4-oxadiazoles, and -imidazolyl-1,3,4-oxadiazoles were synthesized from the synthetic intermediates, methyl 2-((4-aryloxazol-2- ylcarbamoyl)methylsulfonyl)acetate, methyl 2-((4-arylthiazol-2-ylcarbamoyl) methylsulfonyl)acetate, and methyl 2-((4-aryl-1H-imidazol-2-ylcarbamoyl) methylsulfonyl)acetate. All the title compounds were tested for their antioxidant activity. The oxadiazolylmethylsulfonyloxazolylacetamide displayed excellent radical-scavenging activity when compared with the standard ascorbic acid. A new class of acetamidomethylsulfonyl bis heterocycles-oxazolyl/ thiazolyl/imidazolyl-1,3,4-oxadiazoles were synthesized and tested for their antioxidant activity. The oxadiazolylmethylsulfonyloxazolylacetamide displayed excellent radical-scavenging activity when compared with the standard ascorbic acid.
- Mahaboob Basha, Nabhubygari,Lavanya, Gopala,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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p. 511 - 520
(2013/07/26)
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- Synthesis of 2-[4,5-dimethyl-1-(phenylamino)-1H-imidazol-2-ylthio]-N- (thiazole-2-yl)acetamide derivatives and their anticancer activities
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In this work, 2-(4,5-dimethyl-1-(phenylamino)-1H-imidazol-2-ylthio)-N- (thiazol-2-yl) acetamide derivatives were synthesized by reacting 4,5-dimethyl-1-(phenylamino)-1H-imidazole-2(3H)-thione derivatives with some 2-chloro-N-(thiazol-2-yl)acetamide compou
- Duran, Murat,Demirayak, Seref
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p. 4110 - 4124
(2013/09/02)
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- AMIDE THIAZOLE DERIVATIVE, PREPARATION METHOD AND USES THEREOF
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The present invention relates to the field of the drugs associated with the diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is hydrogen, halogen, C1-C5 alkyl, COOR3 or phenyl, wherein R3 is C1-C5 alkyl; R2 is phenyl, substituted phenyl, 2-furanyl, substituted 2-furanyl, 2-thienyl, substituted 2-thienyl, 2-pyrrolyl, or substituted 2-pyrrolyl.
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Page/Page column 5
(2012/02/04)
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- Substituted thiazoles VI. Synthesis and antitumor activity of new 2-acetamido- and 2 or 3-propanamido-thiazole analogs
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A novel series of 2-acetamido and 2 or 3-propanamido derivatives of 4- or 5-substituted-thiazoles was designed and synthesized. Structure elucidation of the new synthesized compounds was attained by the use of 1H & 13C NMR, and Mass
- El-Messery, Shahenda M.,Hassan, Ghada S.,Al-Omary, Fatmah A.M.,El-Subbagh, Hussein I.
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experimental part
p. 615 - 625
(2012/09/21)
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- Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca2+ overload
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In this study, a series of multipotent phenylthiazole-tacrine hybrids (7a-7e, 8, and 9a-9m) were synthesized and biologically evaluated. Screening results showed that phenylthiazole-tacrine hybrids were potent cholinesterase inhibitors with pIC50/su
- Wang, Yue,Wang, Fang,Guan, Xin-Lei,Wang, Can-Ming,Cao, Hui,Li, Ming-Xing,Chen, Jian-Guo,Jiang, Feng-Chao,Li, Lei,Yu, Jun-Ping
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p. 6513 - 6522,10
(2012/12/11)
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- Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca2+ overload
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In this study, a series of multipotent phenylthiazole-tacrine hybrids (7a-7e, 8, and 9a-9m) were synthesized and biologically evaluated. Screening results showed that phenylthiazole-tacrine hybrids were potent cholinesterase inhibitors with pIC50/su
- Wang, Yue,Wang, Fang,Yu, Jun-Ping,Jiang, Feng-Chao,Guan, Xin-Lei,Wang, Can-Ming,Li, Lei,Cao, Hui,Li, Ming-Xing,Chen, Jian-Guo
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p. 6513 - 6522
(2013/01/14)
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- AMIDE THIAZOLE DERIVATIVE, PREPARATION METHOD AND USES THEREOF
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The present invention relates to the field of drugs associated with treating diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.
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Page/Page column 3
(2011/11/30)
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- Synthesis and antiinflammatory activity of 2,4-disubstituted thiazoles
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New thiazoles were synthesized by treating 2-hydrazinyl-N-(4-phenylthiazol- 2-yl) acetamide (5) with chalcones (7a-7j). The chemical structures of the synthesized compounds were confirmed by means of IR, 1H NMR, Mass spectral data and elemental
- Saravanan,Prakash,Panneer Selvam,Dinesh Kumar,Mayuren
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p. 193 - 194
(2013/09/23)
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- Synthesis and antimicrobial activity of 2-(2′-arylidene-hydrazino- acetyl-amino)-4-phenyl-1,3-thiazoles and 2-[2′-{4″-substituted-aryl- 3″-chloro-2″-oxo-azetidine}-acetyl-amino]-4-phenyl-1,3-thiazoles
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As a part of systematic investigation of synthesis and biological activity, several new 2-(2′-substituted-arylidene-hydrazino-acetyl-amino)-4-phenyl- 1,3-thiazoles, 3 and 2-[2′-{4″-substituted-aryl-3″-chloro- 2″-oxo-azetidine}-acetyl-amino]-4-phenyl-1,3-t
- Sonwane,Srivastava,Srivastava
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p. 633 - 636
(2008/09/19)
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- 2-thiazolylimino/heteroarylimino-5-arylidene-4-thiazolidinones as new agents with SHP-2 inhibitory action
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SHP-2, a nonreceptor protein tyrosine phosphatase encoded by the PTPN11 gene, mediates cell signaling by growth factors and cytokines via the RAS/MAP kinase pathway. Somatic mutations in PTPN11 gene account for approximately 18% of juvenile myelomonocytic
- Geronikaki,Eleftheriou,Vicini,Alam,Dixit,Saxena
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body text
p. 5221 - 5228
(2009/07/01)
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- Some 6-substituted 3-aryl-7-oxothiazolo[4,5-d]pyrimidin-2(3H)-thione derivatives and their antimicrobial activities
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In this study, 3-aryl-6-substituted thiazolopyrimidin-2(3H)-thione derivatives 4 and 6 have been synthesized by reacting thiazolopyrimidines 2 with -bromoacetophenone 3 and 2-chloro-N-(2-thiazolyl)acetamides 5. The structure elucidation of the obtained co
- Demirayak, Seref,Ali, Faten Dali,Osman, Baland Sirvan,Tunali, Yagmur
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p. 1793 - 1803
(2008/02/11)
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- Synthesis and microbiological evaluation of 2-acetanilido-4-arylthiazole derivatives
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A series of compounds have been synthesized by reacting 2-amino 4-arylthiazole with different substituted acetanilides and chloroacetylation of 2-amino 4-arylthiazole or their substituted derivatives. Ten different substituted compounds synthesized out of the 2-acetanilido 4-arylthiazole derivatives and 2-pyrazine 4-arylthiazole have been evaluated for the antifungal and antibacterial activities. These compounds have showed moderate antibacterial and very good activity.
- Pattan,Ali, M. Shamrez,Pattan,Purohit,Reddy,Nataraj
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p. 1929 - 1932
(2007/10/03)
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- Synthesis and biological evaluation of new thiazolyl/benzothiazolyl-amides, derivatives of 4-phenyl-piperazine
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A series of thiazolyl-N-phenyl piperazines has been synthesised and tested for anti-inflammatory activity. Their RM values were determined as an expression of their lipophilicity. Theoretical calculation of their lipophilicity, as clog P and logPsk also performed. The effect of the synthesised compounds on inflammation, using the carrageenin induced mouse paw oedema model was studied. In general, the studied compounds were found to be potent anti-inflammatory agents (44-74.1%). Anti-inflammatory activity was influenced by some structural characteristics of the synthesised compounds. An attempt was made to correlate their biological activity with some physicochemical parameters using a quantitative structure-activity relationship approach (QSAR).
- Papadopoulou, Christina,Geronikaki, Athina,Hadjipavlou-Litina, Dimitra
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p. 969 - 973
(2008/09/18)
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- Aminothiazole derivatives with antidegenerative activity on cartilage
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A series of 2-dialkylamino-N-(4-substituted thiazolyl-2)acetamides and 3-dialkylamino-N-(4-substituted thiazolyl-2)propionamides were synthesized and evaluated for their anti-inflammatory activity. Encouraging results led us to investigate the effect of t
- Panico, Anna Maria,Geronikaki, Athina,Mgonzo, Remi,Cardile, Venera,Gentile, Barbara,Doytchinova, Irini
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p. 2983 - 2989
(2007/10/03)
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- Synthesis and biological evaluation of new 4,5-disubstituted-thiazolyl amides, derivatives of 4-hydroxy-piperidine or of 4-N-methyl piperazine
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4,5-disubstituted-thizolyl amides, derivatives of 4-hydroxy-piperidine and of 4-N-methyl piperazine, were synthesized and tested as anti-inflammatory agents. Log P values were theoretically calculated and experimentally determined. These compounds were tested for antioxidant activity, as hydroxyl radical scavengers and for their ability to interact with stable 1,1-diphenyl-2-picryl hydrazyl free radical (DPPH). The effect of the synthesized compounds on inflammation, using the carrageenin induced mice paw edema model was studied. Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesized compounds.
- Geronikaki,Hadjipavlou-Litina,Chatziopoulos,Soloupis
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p. 472 - 479
(2007/10/03)
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- Silyl modification of biologically active compounds. 8. Trimethylsilyl ethers of hydroxyl-containing thiazole derivatives
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Trimethylsilyl ethers of various hydroxyl-containing thiazole derivatives have been synthesized. The psychotropic activity (in vivo) and the cytotoxicity (in vitro on tumor cell lines HT-1080 and MG-22A) of these ethers and of their unsilylated precursors
- Zablotskaya,Segal,Germane,Shestakova,Domracheva,Nesterova,Geronikaki,Lukevics
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p. 859 - 866
(2007/10/03)
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- Synthesis and fungicidal activity of 2-imino-3-(4-arylthiazol-2-yl)- thiazolidin-4-ones and their 5-arylidene derivatives
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Five derivatives of 2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones and a series of their 5-arylidene derivatives have been synthesized and tested for antifungal activity against seven agricultural fungi. 2-Imino-3-(2,4-dichloro-5- fluorophenylthiazol-2-yl)-4-thiazolidi-none and 2-imino-3-(2,4- dichlorophenylthiazol-2-yl)-4-thiazolidione, both of them new compounds, exhibited higher fungicidal effects than the other compounds prepared.
- Liu, Hui-Ling,Li, Zongcheng,Anthonsen, Thorleif
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p. 1055 - 1061
(2007/10/03)
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- SYNTHESIS AND TRANSFORMATIONS OF 4-SUBSTITUTED 2-AMINOTHIAZOLES
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4-Substituted 2-aminothiazoles were synthesized and some of the transformations of these compounds at the amino group were studied.A number of new thiazole derivatives were obtained.
- Ibatullin, U. G.,Petrushina, T. F.,Leitis, L. Ya,Minibaev, I. Z.,Logvin, B. O.
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p. 612 - 616
(2007/10/02)
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- Synthesis of 2-(aminoacetylamino)thiazole derivatives and comparison of their local anaesthetic activity by the method of action potential
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Some numbers of the family of 2-(aminoacetylamino)thiazoles were synthesized. The structure of these compounds was identified both by elemental as well as by spectroscopic analysis (UV, IR, H-NMR, MS). The possible local anaesthetic action of these compounds was also tested using the sciatic nerve of the frog. None of the tested compounds were found to have local anaesthetic action on in vitro preparations as lidocaine, but one of the compounds showed a similar anaesthetic action to procaine.
- Geronikaki,Theophilidis
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p. 709 - 716
(2007/10/02)
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