新型苯基(2h -四唑-5-基)甲烷胺衍生物的设计、合成和抗真菌活性评价。

Amol B Salake, Aparna S Chothe, Shrikant S Nilewar, Madhavi Khilare, Rutuja S Meshram, Abhishek A Pandey, M K Kathiravan
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引用次数: 8

摘要

真菌感染对人类健康和生命构成持续而严重的威胁。在许多属的真菌中都观察到内在抗性。许多真菌感染是由机会性病原体引起的,可能是内源性的(念珠菌感染)或从环境中获得的(隐球菌和曲霉菌感染)。因此,需要新的治疗策略来对抗各种真菌感染。氟康唑具有良好的抗真菌活性,毒性较低,是首选的一线抗真菌药物,但存在严重的耐药问题。因此,有必要通过对类氟康唑结构的修饰来设计新型的类似物。以α-氨基腈为原料,在异丙醇的存在下,与叠氮化钠和氯化锌反应,合成了一系列新的苯基(2h -四唑-5-基)甲胺衍生物。测定了它们对白色念珠菌和黑曲霉的抗真菌活性,并进行了对1EA1的对接研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, synthesis, and evaluations of antifungal activity of novel phenyl(2H-tetrazol-5-yl)methanamine derivatives.

Fungal infections pose a continuous and serious threat to human health and life. The intrinsic resistance has been observed in many genera of fungi. Many fungal infections are caused by opportunistic pathogens that may be endogenous (Candida infections) or acquired from the environment (Cryptococcus and Aspergillus infections). So, new therapeutic strategies are needed to combat various fungal infections. Fluconazole shows good antifungal activity with relatively low toxicity and is preferred as first line antifungal therapy, but it has suffered from severe drug resistance. So, there is a need to design novel analogues by modification of fluconazole-like structure. A novel series of phenyl(2H-tetrazol-5-yl)methanamine derivatives were synthesized by reaction of α-amino nitrile with sodium azide and ZnCl2 in presence of isopropyl alcohol. They were evaluated for antifungal activity against Candida albicans and Aspergillus niger and subjected to docking study against 1EA1.

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