Discovery of a Novel Broad-Spectrum Antifungal Agent Derived from Albaconazole
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- 作者：R茅mi Guillon ; Fabrice Pagniez ; Carine Picot ; Damien H茅dou ; Alain Tonnerre ; Elizabeth Chosson ; Muriel Duflos ; Thierry Besson ; C茅dric Log茅 ; Patrice Le Pape
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：February 14, 2013
- 年：2013
- 卷：4
- 期：2
- 页码：288-292
- 全文大小：284K
- 年卷期：v.4,no.2(February 14, 2013)
- ISSN：1948-5875
文摘
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.