新型氟苯并咪唑类抗菌及抗真菌药物的合成与评价

D. Joshi, R. Narigara, G. Jani, K. Parikh
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引用次数: 0

摘要

合成了一类新的氟苯并咪唑衍生物(IIIa-j),研究了它们的抗菌潜力。所有化合物均由5-(二氟甲氧基)- 1h -苯并咪唑-2-硫醇(I)的合成开始,通过多步合成得到。化合物I进一步与不同取代苯胺与氯乙酰氯和三乙胺在DMF(溶剂)中反应得到的2-氯- n -苯乙酰胺(IIa-j)的不同衍生物进行反应;从而形成氟苯并咪唑IIIa-j。通过1H NMR、13C NMR、质谱、元素分析和IR对化合物IIIa-j进行了表征。所有化合物对革兰氏阳性菌(金黄色葡萄球菌和粪肠球菌)和革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)以及真菌(黑杆菌和白色念珠菌)的抑菌活性进行了体外筛选。其中一些化合物在抗革兰氏阴性菌株的MIC中表现出良好的效果。
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 Evaluation of Novel Fluorobenzimidazole Derivatives as Antibacterial and Antifungal Agents
A new class of fluorobenzimidazole derivatives (IIIa-j)was synthesized to investigate their antimicrobial potential. All the compounds were prepared by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol (I). The compound I was further reacted with different derivatives of 2-chloro-N-phenylacetamide (IIa-j) prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF (solvent); resulting in formation of fluorobenzimidazoles IIIa-j. The compounds IIIa-j were characterized by spectral analysis viz. 1H NMR, 13C NMR, mass spectra, elemental analysis and IR. All these compounds were screened in vitro for their antimicrobial activity against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans). Some of the compounds exhibited promising results (in MIC) against Gram-negative bacterial strains.
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