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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and preliminary evaluation of benzimidazole derivatives as antimicrobial agents.
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Synthesis and preliminary evaluation of benzimidazole derivatives as antimicrobial agents.

机译：苯并咪唑衍生物作为抗菌剂的合成与初步评价。

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摘要

A series of 2-alkylsulphanylbenzimidazoles was synthesised and the compounds were evaluated for their in vitro antimicrobial activity. The structures of the compounds were confirmed by 1H-NMR and IR data, and their purity by elemental analysis. Antimycobacterial activities against Mycobacterium tuberculosis and non-tuberculous mycobacteria as well as antifungal activities against Candida albicans, Candida tropicalis, Candida krusei, Candida glabrata, Trichosporon beigelii, Trichophyton mentagrophytes and Aspergillus fumigatus were expressed as the corresponding MIC values. The substances exhibited appreciable antimycobacterial activity, in particular, against non-tuberculous mycobacteria. The activity of the most active compound in the set, 3,5-dinitro derivative 4t, exceeded that of the standard isoniazide against M. kansasii and M. avium. The antifungal activities of the compounds were relatively low. A weak antifungal effect was observed against the dermatophyte Trichophyton mentagrophytes. None of the compounds showed significant inhibitory activity against yeasts.
机译：合成了一系列的2-烷基磺酰基苯并咪唑，并评估了这些化合物的体外抗菌活性。化合物的结构通过1 H-NMR和IR数据确认，其纯度通过元素分析确认。分别表示了对结核分枝杆菌和非结核分枝杆菌的抗分枝杆菌活性以及对白色念珠菌，热带念珠菌，克鲁斯念珠菌，光滑念珠菌，米氏曲霉，米氏毛癣菌和烟曲霉的抗真菌活性。这些物质表现出明显的抗分枝杆菌活性，特别是针对非结核性分枝杆菌。该组中活性最高的化合物3,5-二硝基衍生物4t的活性超过了标准异烟肼对堪萨斯分枝杆菌和鸟分枝杆菌的活性。该化合物的抗真菌活性相对较低。观察到对皮肤癣菌Trichophyton mentagrophytes的抗真菌作用较弱。这些化合物均未显示出对酵母的显着抑制活性。

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