Design and optimization of highly-selective fungal CYP51 inhibitors

While the orally-active azoles such as voriconazole and itraconazole are effective antifungal agents, they potently inhibit a broad range of off-target human cytochrome P450 enzymes (CYPs) leading to various safety issues (e.g., drug-drug interactions, liver toxicity). Herein, we describe rationally...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-08, Vol.24 (15), p.3455-3458
Hauptverfasser:	Hoekstra, William J, Garvey, Edward P, Moore, William R, Rafferty, Stephen W, Yates, Christopher M, Schotzinger, Robert J
Format:	Artikel
Sprache:	eng
Schlagworte:	14-alpha Demethylase Inhibitors - chemical synthesis 14-alpha Demethylase Inhibitors - chemistry 14-alpha Demethylase Inhibitors - pharmacology Antifungal Agents - chemical synthesis Antifungal Agents - chemistry Antifungal Agents - pharmacology Candida albicans - drug effects Candida albicans - enzymology Candida albicans - growth & development Dose-Response Relationship, Drug Drug Design Microbial Sensitivity Tests Molecular Conformation Sterol 14-Demethylase - metabolism Structure-Activity Relationship
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