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Discovery of a Novel Broad-Spectrum Antifungal Agent Derived from Albaconazole

机译:发现一种新型的广谱抗真菌剂,来自阿尔巴康唑

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摘要

Synthesis of a strict structural analogue of albaconazole in which the quinazolinone ring is fused by a thiazole moiety led to the discovery of a new triazole with broad-spectrum antifungal activity. Compound I exhibited high in vitro activity against pathogenic Candida species and filamentous fungi and showed preliminary in vivo antifungal efficacy in a mice model of systemic candidiasis.
机译:严格合成阿尔巴康唑的结构类似物,其中喹唑啉酮环被噻唑部分稠合,导致发现了具有广谱抗真菌活性的新三唑。化合物I对致病性念珠菌和丝状真菌表现出很高的体外活性,并且在系统性念珠菌病小鼠模型中显示出初步的体内抗真菌功效。

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