| Literature DB >> 27180013 |
Wensheng Yu1, Craig A Coburn2, De-Yi Yang3, Peter T Meinke3, Michael Wong3, Stuart B Rosenblum3, Kevin X Chen3, George F Njoroge3, Lei Chen3, Michael P Dwyer3, Yueheng Jiang3, Anilkumar G Nair3, Oleg Selyutin3, Ling Tong3, Qingbei Zeng3, Bin Zhong4, Tao Ji4, Bin Hu4, Sony Agrawal5, Ellen Xia5, Ying Zhai5, Rong Liu6, Rong Kong6, Paul Ingravallo6, Ernest Asante-Appiah6, Amin Nomeir7, James Fells8, Joseph A Kozlowski3.
Abstract
HCV NS5A inhibitors have demonstrated impressive in vitro potency profiles in HCV replicon assays and robust HCV RNA titer reduction in the clinic making them attractive components for inclusion in an all oral fixed dose combination regimen for the treatment of HCV infection. Herein, we describe research efforts that led to the discovery of a series of fused tricyclic core containing HCV NS5A inhibitors such as 24, 39, 40, 43, and 44 which have pan-genotype activity and are orally bioavailable in the rat.Entities:
Keywords: Direct-acting antiviral agents (DAA); Elbasvir; HCV NS5A inhibitor; Hepatitis C; Pan-genotype activity; Tricyclic
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Year: 2016 PMID： 27180013 DOI： 10.1016/j.bmcl.2016.04.084
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823