St. Johns Pharmacy College, Department of Medicinal Chemistry, 6, 2nd stage Vijaynagar, R.P.C. Layout, Bangalore 560040, Karnataka, India.
Eur J Med Chem. 2010 May;45(5):2063-74. doi: 10.1016/j.ejmech.2010.01.045. Epub 2010 Jan 28.
In the present study a series of 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazole derivatives have been synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral analysis. Synthesized compounds were evaluated for their preliminary cytotoxicity, antimicrobial and antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Antimycobacterial activity tested against M. tuberculosis indicated that compounds 4b and 6g exhibited twofold enhanced potency than parent compound 1 and the results indicate that some of them exhibited promising activities and they deserve more consideration as potential antitubercular agents. Compound 3c, 4b and 6c exhibited good or moderate antibacterial inhibition and compounds 3h and 7c showed excellent antifungal activity.
在本研究中，一系列 2-取代-5-[异丙基噻唑]稠合的 1,2,4-三唑和 1,3,4-噁二唑衍生物已被合成并通过红外光谱、1H NMR、13C NMR 和质谱分析进行了表征。通过肉汤稀释法评估了合成化合物的初步细胞毒性、抗微生物和抗结核活性，以结核分枝杆菌 H37Rv 株为研究对象。抗结核活性测试表明，化合物 4b 和 6g 的活性比母体化合物 1 增强了两倍，结果表明其中一些化合物具有良好的活性，值得进一步研究作为潜在的抗结核药物。化合物 3c、4b 和 6c 表现出良好或中等的抗菌抑制作用，化合物 3h 和 7c 表现出优异的抗真菌活性。
