Discovery of ravidasvir (PPI-668) as a potent pan-genotypic HCV NS5A inhibitor

  • Bioorg Med Chem Lett. 2016 Sep 15;26(18):4508-4512. doi: 10.1016/j.bmcl.2016.07.066.
Min Zhong  1 ,  Eric Peng  2 ,  Ningwu Huang  2 ,  Qi Huang  2 ,  Anja Huq  2 ,  Meiyen Lau  2 ,  Richard Colonno  2 ,  Leping Li  3
Affiliations
  • 1. Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. Electronic address: [email protected].
  • 2. Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA.
  • 3. Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. Electronic address: [email protected].
PMID: 27506559 DOI: 10.1016/j.bmcl.2016.07.066
Abstract

This Letter describes the synthesis, representative structure activity relationship (SAR), activity and PK profiles of a series of functionalized benzimidazole-naphthylene-imidazole derivatives as HCV NS5A inhibitors. This effort successfully led to the discovery of ravidasvir (PPI-668), which has been well tolerated and shown high sustained viral response rates as a key component in all-oral combination regimens in multiple human clinical trials.

Keywords
Benzimidazole–naphthylene–imidazole derivatives; Hepatitis C virus; NS5A inhibitor; PPI-668; Ravidasvir.
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