Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity. Academic Article uri icon

Overview

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.

authors

  • Yu, Wensheng
  • Coburn, Craig A
  • Yang, De-Yi
  • Meinke, Peter T
  • Wong, Michael
  • Rosenblum, Stuart B
  • Chen, Kevin X
  • Njoroge, George F
  • Chen, Lei
  • Dwyer, Michael P
  • Jiang, Yueheng
  • Nair, Anilkumar G
  • Selyutin, Oleg
  • Tong, Ling
  • Zeng, Qingbei
  • Zhong, Bin
  • Ji, Tao
  • Hu, Bin
  • Agrawal, Sony
  • Xia, Ellen
  • Zhai, Ying
  • Liu, Rong
  • Kong, Rong
  • Ingravallo, Paul
  • Asante-Appiah, Ernest
  • Nomeir, Amin
  • Fells, James
  • Kozlowski, Joseph A

publication date

  • April 30, 2016

Research

keywords

  • Antiviral Agents
  • Drug Discovery
  • Hepacivirus
  • Hepatitis C
  • Viral Nonstructural Proteins

Identity

Scopus Document Identifier

  • 84970038690

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2016.04.084

PubMed ID

  • 27180013

Additional Document Info

volume

  • 26

issue

  • 13