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首页> 外文期刊>Journal of Advanced Research >Butenafine and analogues: An expeditious synthesis and cytotoxicity and antifungal activities
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Butenafine and analogues: An expeditious synthesis and cytotoxicity and antifungal activities

机译：Butenafine及其类似物：快速合成，细胞毒性和抗真菌活性

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The incidence of fungal infections is considered a serious public health problem worldwide. The limited number of antimycotic drugs available to treat human and animal mycosis, the undesirable side effects and toxicities of the currently available drugs, and the emergence of fungal resistance emphasizes the urgent need for more effective antimycotic medicines. In this paper, we describe a rapid, simple, and efficient synthetic route for preparation of the antifungal agent butenafine on a multigram scale. This novel synthetic route also facilitated the preparation of 17 butenafine analogues using Schiff bases as precursors in three steps or less. All the synthesized compounds were evaluated against the yeast, Cryptococcus neoformans / C. gattii species complexes and the filamentous fungi Trichophyton rubrum and Microsporum gypseum . Amine 4bd , a demethylated analogue of butenafine, and its corresponding hydrochloride salt showed low toxicity in vitro and in vivo while maintaining inhibitory activity against filamentous fungi.
机译：真菌感染的发生率被认为是世界范围内的严重公共卫生问题。可用于治疗人和动物真菌病的抗真菌药数量有限，目前可用药物的不良副作用和毒性以及真菌抗药性的出现凸显了对更有效抗真菌药的迫切需求。在本文中，我们描述了一种快速，简单，有效的合成路线，以克为单位制备抗真菌剂丁烯那芬。这种新颖的合成路线还促进了使用Schiff碱作为前体的三个步骤或更少步骤的制备17个丁那芬类似物。对所有合成的化合物进行了针对酵母，新隐球菌/加迪梭菌物种复合物以及丝状真菌毛癣菌和小孢子菌的评估。丁那芬的脱甲基类似物胺4bd及其相应的盐酸盐在保持体内对丝状真菌的抑制活性的同时，在体内和体外均显示出低毒性。

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