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

…, C Callebaut, YC Choi, MS Lee, J Chau, LK Tsai…

Index: Xu, Lianhong; Liu, Hongtao; Hong, Allen; Vivian, Randy; Murray, Bernard P.; Callebaut, Christian; Choi, You-Chul; Lee, Melody S.; Chau, Jennifer; Tsai, Luong K.; Stray, Kirsten M.; Strickley, Robert G.; Wang, Jianhong; Tong, Leah; Swaminathan, Swami; Rhodes, Gerry R.; Desai, Manoj C. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 3 p. 995 - 999

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Citation Number: 8

Abstract

Abstract The HIV protease inhibitor (PI) ritonavir (RTV) has been widely used as a pharmacoenhancer for other PIs, which are substrates of cytochrome P450 3A (CYP3A). However the potent anti-HIV activity of ritonavir may limit its use as a pharmacoenhancer with other classes of anti-HIV agents. Ritonavir is also associated with limitations such as poor physicochemical properties. To address these issues a series of compounds with ...