P. G. Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad, India.
Arch Pharm (Weinheim). 2011 May;344(5):311-9. doi: 10.1002/ardp.200900291. Epub 2011 Jan 31.
A series of novel 2-(1H-benzimidazol-2-ylsulfanyl)-N-(4-oxo-2-phenyl-thiazolidin-3yl)-acetamide 5a-j have been synthesized from various aldehydes and 2-(5-phenyl-[1,3,4]-oxadiazol-2-ylmethylsulfanyl)-1H-benzimidazole 6a-j from various benzoic acids. These compounds were screened for their in-vitro anti-bacterial activity against Staphylococcus aureus and Enterococcus faecalis as Gram positive, Klebsiella pneumoniae and Escherichia coli as Gram negative bacterial strains and for in-vitro anti-fungal activity against Asperigillus fumigatus and Candida albicans. The in vitro cytotoxic properties were studied using brine shrimp bioassay. Results revealed that, compounds 5b, 5d, 5g, 5i, 6b, 6e, 6f, and 6i showed excellent activity against a panel of microorganisms. The cytotoxic activities of 5b, 5g, 5i, 6b, 6f, 6h, and 6i were found to be good. All the newly synthesized compounds were characterized by elemental analysis, IR, (1)H-NMR, (13)C-NMR and MS.
已经从各种醛和 2-(5-苯基-[1,3,4]-恶二唑-2-基甲基硫代)-1H-苯并咪唑 6a-j 合成了一系列新型 2-(1H-苯并咪唑-2-基硫代)-N-(4-氧代-2-苯基-噻唑烷-3-基)-乙酰胺 5a-j。这些化合物被筛选出对金黄色葡萄球菌和粪肠球菌作为革兰氏阳性菌、肺炎克雷伯菌和大肠杆菌作为革兰氏阴性菌的体外抗菌活性，以及对烟曲霉和白色念珠菌的体外抗真菌活性。体外细胞毒性性质使用盐水虾生物测定法进行研究。结果表明，化合物 5b、5d、5g、5i、6b、6e、6f 和 6i 对一组微生物表现出优异的活性。5b、5g、5i、6b、6f、6h 和 6i 的细胞毒性活性被发现良好。所有新合成的化合物均通过元素分析、IR、(1)H-NMR、(13)C-NMR 和 MS 进行了表征。
