Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors

…, W Schepens, S Hallenberger, J Baumeister…

Index: Jonckers, Tim H.M.; Rouan, Marie-Claude; Hache, Geerwin; Schepens, Wim; Hallenberger, Sabine; Baumeister, Judith; Sasaki, Jennifer C. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 4998 - 5002

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Citation Number: 9

Abstract

A new class of benzoxazole and benzothiazole amide derivatives exhibiting potent CYP3A4 inhibiting properties was identified. Extensive lead optimization was aimed at improving the CYP3A4 inhibitory properties as well as overall ADME profile of these amide derivatives. This led to the identification of thiazol-5-ylmethyl (2S, 3R)-4-(2-(ethyl (methyl) amino)-N- isobutylbenzo [d] oxazole-6-carboxamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate (C1) ...