Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents

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• 作者：Francis Giraud ; Cé ; dric Logé ; Fabrice Pagniez ; Damien Crepin ; Patrice Le Pape ; Marc Le Borgne
• 关键词：Homology model ; Docking ; H-bond acceptor ; Triazole ; Oxirane ; Azide ; Microwave irradiation ; Candida albicans ; CYP51 inhibitors ; Antifungal agents
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March 2008
• 卷：18
• 期：6
• 页码：1820-1824
• 文件大小：234 K

摘要

A series of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols 6a–c, 7a–c, 8a, and 9a were prepared in five steps and evaluated for their antifungal activity. The most active compound 7b was docked into a home-made 3D model of the targeted enzyme confirming the importance of Tyr118, His377, and Ser378 residues in its binding mode.