含苯并噻唑和苯二氮卓的1,3,4-恶二唑的合成及生物学评价

P. Navin, Patel Sarvil, P. Amit, P. Divyesh, Rajani Dhansukh, R. Moo-Puc, G. Rivera
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引用次数: 8

摘要

摘要合成了一系列含有1,3,4-恶二唑片段的噻唑类药物和二氮类药物,分析了它们对几种细菌(金黄色葡萄球菌、化脓性葡萄球菌、大肠杆菌、铜绿假单胞菌)、真菌(白色念珠菌、黑曲霉、克拉曲霉)和原虫(溶组织内阿米巴、兰贾第鞭毛虫、克氏锥虫和墨西哥利什曼原虫)的体外抑菌活性。所选化合物中很少有抗结核活性。然而,人们注意到,最终类似物对每种菌株的效力取决于恶二唑芳基环上取代基的类型,以及苯并噻唑类和苯二氮卓类药物中噻吩、吡啶和呋喃的存在。生物学筛选发现部分化合物具有良好的抗菌和抗结核活性(MIC值为62.5 ~ 100 μg/mL)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties
Abstract A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on aryl ring of oxadiazole as well as presence of thiophene, pyridine, and furan at benzothiazepines and benzodiazepines. The biological screening identified that some of the compounds were found to possess good antimicrobial and antitubercular (62.5–100 μg/mL of MIC) activity.
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