Article
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Bioorganic & medicinal chemistry letters - 1 Mar 2016
Nair Anilkumar G, Zeng Qingbei, Selyutin Oleg, Rosenblum Stuart B, Jiang Yueheng, Yang De-Yi, Keertikar Kerry, Zhou Guowei, Dwyer Michael P, Kim Seong Heon, Shankar Bandarpalle, Yu Wensheng, Tong Ling, Chen Lei, Mazzola Robert, Caldwell John, Tang Haiqun, Allard Melissa L, Buckle Ronald N, Gauuan Polivina Jolicia F, Holst Christian L, Martin Gregory S, Naicker Kannan P, Vellekoop Samuel, Agrawal Sony, Liu Rong, Kong Rong, Ingravallo Paul, Xia Ellen, Zhai Ying, Nomeir Amin, Kozlowski Joseph A
Abstract excerpt
HCV NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays thus making them attractive components for inclusion in an all oral fixed dose combination treatment regimen. Herein we describe the research efforts that led to the discovery of silyl proline containing HCV NS5A inhibitors such as 7e and 8a with pan-genotype activity profile and acceptable pharmacokinetic properties.
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