Discovery of MK??8742: An HCV NS5A Inhibitor with Broad Genotype Activity

…, S Kargman, J Kozlowski, R Liu, JA McCauley…

Index: Coburn, Craig A.; Meinke, Peter T.; Chang, Wei; Fandozzi, Christine M.; Graham, Donald J.; Hu, Bin; Huang, Qian; Kargman, Stacia; Kozlowski, Joseph; Liu, Rong; McCauley, John A.; Nomeir, Amin A.; Soll, Richard M.; Vacca, Joseph P.; Wang, Dahai; Wu, Hao; Zhong, Bin; Olsen, David B.; Ludmerer, Steven W. ChemMedChem, 2013 , vol. 8, # 12 p. 1930 - 1940

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Citation Number: 84

Abstract

Abstract The NS5A protein plays a critical role in the replication of HCV and has been the focus of numerous research efforts over the past few years. NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays, making them attractive components for inclusion in all oral combination regimens. Early work in the NS5A arena led to the discovery of our first clinical candidate, MK-4882 [2-((S)-pyrrolidin-2-yl)-5-(2-(4-(5-(( ...