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Synthesis, antimicrobial activity and cytotoxicity of 2-substituted benzimidazole incorporated with thiazole
Indian Journal of Chemistry, Section B ( IF 0.456 ) Pub Date : 2021-11-16
Chirag R Fultariya, Jalpa P Harsora

Two new series 2-(2-(1-(1-methyl-1H-benzo[d]imidazol-2-yl)ethylidene)hydrazinyl)-4-(aryl)thiazoles 3a-k and 2-(2-(1- (1-methyl-1H-benzo[d]imidazol-2-yl)ethyl)hydrazinyl)-4-(aryl)thiazoles 4a-k encompassing benzimidazole incorporated with thiazole have been synthesized using rational approach. These thiazole derivatives 3a-k have been reduced at the site of formation of Schiff base (>CH=N−) to obtain final compounds 4a-k. Compounds 3a-k and 4a-k have been screened for their in vitro antibacterial and antifungal actions against four strains each. Among the screened compounds, 3d, 3e, 3f, 3g, 3j, 3k, 4d, 4e, 4f and 4k have emerged as highly effective antibacterial agents, while compounds 3d, 3e, 3f, 3k and 4k have come out as most potent antifungal molecules. Comparison of outcomes of antibacterial and antifungal screening of compounds 3a-k and 4a-k directed that antimicrobial potential of unreduced derivatives 3a-k is higher than reduced derivatives 4a-k. SAR study reveals that presence of halogen (-F, -Cl, -Br) substituents is accountable for significant antimicrobial potential. Also the results of preliminary MTT cytotoxicity assay on HeLa cells indicates that antimicrobial activity of 3e, 3f, 3g, 3j, 3k, 4e, 4f and 4k is accompanied by low extent of cytotoxic concentrations.

中文翻译:

与噻唑结合的2-取代苯并咪唑的合成、抗菌活性和细胞毒性

两个新系列 2-(2-(1-(1-methyl-1H-benzo[d]imidazol-2-yl)ethylidene)hydrazinyl)-4-(aryl)thiazoles 3a-k 和 2-(2-(1 - (1-甲基-1H-苯并[d]咪唑-2-基)乙基)肼基)-4-(芳基)噻唑4a-k包括与噻唑结合的苯并咪唑已使用合理方法合成。这些噻唑衍生物 3a-k 在形成席夫碱 (>CH=N-) 的位置被还原以获得最终化合物 4a-k。已筛选化合物 3a-k 和 4a-k 分别对四种菌株的体外抗菌和抗真菌作用。在筛选的化合物中,3d、3e、3f、3g、3j、3k、4d、4e、4f和4k已成为高效抗菌剂,而化合物3d、3e、3f、3k和4k已成为最有效的抗真菌剂分子。化合物 3a-k 和 4a-k 的抗菌和抗真菌筛选结果的比较表明未还原衍生物 3a-k 的抗菌潜力高于还原衍生物 4a-k。SAR 研究表明,卤素(-F、-Cl、-Br)取代基的存在是产生显着抗菌潜力的原因。此外,对 HeLa 细胞的初步 MTT 细胞毒性测定结果表明,3e、3f、3g、3j、3k、4e、4f 和 4k 的抗菌活性伴随着低程度的细胞毒性浓度。
更新日期:2021-11-16
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