4.5 Article

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

期刊

ACS MEDICINAL CHEMISTRY LETTERS
卷 4, 期 2, 页码 288-292

出版社

AMER CHEMICAL SOC
DOI: 10.1021/ml300429p

关键词

Candida; Aspergillus; zygomycetes; antifungal agents; azoles; thiazolo[4,5-g]quinazolin-8(7H)-one

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  1. Ministere de l'Enseignement Superieur et de la Recherche (MESR)

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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.

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