Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350).

Lianhong Xu,Hongtao Liu,Allen Hong,Randy Vivian,Bernard P Murray,Christian Callebaut,You-Chul Choi,Melody S Lee,Jennifer Chau,Luong K Tsai,Kirsten M Stray,Robert G Strickley,Jianhong Wang,Leah Tong,Swami Swaminathan,Gerry R Rhodes,Manoj C Desai

Bioorganic & Medicinal Chemistry Letters（2014）

引用 25|浏览14

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摘要

A series of novel 1,4-diamine-based CYP3A inhibitors were designed and evaluated. A potent and selective inhibitor of CYP3A, cobicistat (35, GS-9350) was discovered as a novel pharmacoenhancer.

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关键词

CYP3A inhibitors,1,4-Diamines,Pharmacoenhancer,Selectivity against different CYP enzymes

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