Literature DB >> 27506559

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

Min Zhong1, Eric Peng2, Ningwu Huang2, Qi Huang2, Anja Huq2, Meiyen Lau2, Richard Colonno2, Leping Li3.   

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.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh：

Substances：

Year:  2016        PMID： 27506559     DOI： 10.1016/j.bmcl.2016.07.066

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Monte Carlo Method and GA-MLR-Based QSAR Modeling of NS5A Inhibitors against the Hepatitis C Virus.

Authors:  Wissal Liman; Mehdi Oubahmane; Ismail Hdoufane; Imane Bjij; Didier Villemin; Rachid Daoud; Driss Cherqaoui; Achraf El Allali
Journal:  Molecules       Date:  2022-04-23       Impact factor: 4.927

2.  Efficacy of a 12-Week Simeprevir Plus Peginterferon/Ribavirin (PR) Regimen in Treatment-Naïve Patients with Hepatitis C Virus (HCV) Genotype 4 (GT4) Infection and Mild-To-Moderate Fibrosis Displaying Early On-Treatment Virologic Response.

Authors:  Tarik Asselah; Christophe Moreno; Christoph Sarrazin; Michael Gschwantler; Graham R Foster; Antonio Craxí; Peter Buggisch; Faisal Sanai; Ceyhun Bicer; Oliver Lenz; Gino Van Dooren; Catherine Nalpas; Isabelle Lonjon-Domanec; Michael Schlag; Maria Buti
Journal:  PLoS One       Date:  2017-01-05       Impact factor: 3.240

Review 3.  Current therapy for chronic hepatitis C: The role of direct-acting antivirals.

Authors:  Guangdi Li; Erik De Clercq
Journal:  Antiviral Res       Date:  2017-02-24       Impact factor: 5.970

4.  Pharmacokinetics, Safety, and Tolerability of Ravidasvir, with and without Danoprevir/Ritonavir, in Healthy Subjects.

Authors:  Guolan Wu; Huili Zhou; Jing Wu; Duo Lv; Lihua Wu; You Zhai; Meihua Lin; Jingzi J Wu; Jianzhong Shentu
Journal:  Antimicrob Agents Chemother       Date:  2021-07-12       Impact factor: 5.191
  4 in total

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