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Mukunda R. Patekar Vijay J. Medhane Ghanshyam J. Jadhav Mayur J. Thakare Dattatray G. Deshmukh 《Journal of heterocyclic chemistry》2021,58(11):2152-2162
A new series of (s)-1-{3-[4-(4-benzo[d]isothiazol-3-yl-piperazin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmetyl}-3-substituted-urea derivatives have been synthesized and characterized with spectral data, such as IR, NMR and Mass spectroscopies. All compounds are in vitro evaluated for their efficacy as antimicrobial agent against the gram-positive pathogenic strains such as Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228 and Streptococcus pyogens ATCC 8668. Five compounds ( 19k , 19l , 19m , 19n and 19o ) out of 15 compounds showed moderate activity. 相似文献
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Xing Zhou LI Xian Ping DAI Jun Hai XIAO Song LI* Beijing Institute of Pharmacology & Toxicology Beijing School of pharmaceutical Engineering Shenyang Pharmaceutical University Shengyang 《中国化学快报》2005,16(9):1137-1139
For discovering novel small molecule inhibitors of transforming growth factor-β1(TGF-β1)type-I receptor(ALK5),we designed1,3,5-triaryl-4-hydroxyl-4,5-dihydro-1H-pyrazole(1)as target compound,mimic the structure of SB-431542which is a2-pyridyl substituted triarylimiazole inhibitor of ALK51.Racemic compound1showed moderate ALK5inhibitory activity in luciferase reporter assays[inhibition(%control):0.1umol/L8.79%;1umol/L19.05%].To investigate the influence of the absolute configuration of… 相似文献
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Herein, an excellent method for the synthesis of twelve novel Schiff base derivatives containing indole and triazole assisted by microwave irradiation is reported. Compared with the conventional method, the yields increased from 59–84 % to 85–96 % and the reaction time was reduced from 24–30 h to 4–8 min. Moreover, all series of the newly synthesized Schiff bases were evaluated for their antibacterial activity. The values of minimum inhibitory concentration (MIC) and IC50 indicated that many target compounds possessed excellent antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Bacillus subtilis. 相似文献
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A series of novel 1-[(2,6-dichloro-4-trifluoromethyl)phenyl]-3-aryl-1H-pyrazole-4-carbaldehydes were synthesized using the Vilsmeier-Haack reagent. The structures of all the title compounds have been confirmed by elemental analysis, 1H-NMR and 13C-NMR and in addition, the structure of intermediate 5b was investigated by X-ray crystallography. 相似文献