Literature DB >> 22366653

Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.

X Christopher Sheng1, Todd Appleby, Thomas Butler, Ruby Cai, Xiaowu Chen, Aesop Cho, Michael O Clarke, Jeromy Cottell, William E Delaney, Edward Doerffler, John Link, Mingzhe Ji, Rowchanak Pakdaman, Hyung-Jung Pyun, Qiaoyin Wu, Jie Xu, Choung U Kim.   

Abstract

The discovery of GS-9451 is reported. Modification of the P3 cap and P2 quinoline with a series of solubilizing groups led to the identification of potent HCV NS3 protease inhibitors with greatly improved pharmacokinetic properties in rats, dogs and monkeys.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22366653     DOI: 10.1016/j.bmcl.2012.01.017

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


  8 in total

Review 1.  Hepatitis C virus molecular evolution: transmission, disease progression and antiviral therapy.

Authors:  Maria Victoria Preciado; Pamela Valva; Alejandro Escobar-Gutierrez; Paula Rahal; Karina Ruiz-Tovar; Lilian Yamasaki; Carlos Vazquez-Chacon; Armando Martinez-Guarneros; Juan Carlos Carpio-Pedroza; Salvador Fonseca-Coronado; Mayra Cruz-Rivera
Journal:  World J Gastroenterol       Date:  2014-11-21       Impact factor: 5.742

2.  Robust and persistent replication of the genotype 6a hepatitis C virus replicon in cell culture.

Authors:  Mei Yu; Betty Peng; Katie Chan; Ruoyu Gong; Huiling Yang; William Delaney; Guofeng Cheng
Journal:  Antimicrob Agents Chemother       Date:  2014-02-18       Impact factor: 5.191

3.  Characterization of resistance to the protease inhibitor GS-9451 in hepatitis C virus-infected patients.

Authors:  Hadas Dvory-Sobol; Kelly A Wong; Karin S Ku; Andrew Bae; Eric J Lawitz; Phillip S Pang; Jeanette Harris; Michael D Miller; Hongmei Mo
Journal:  Antimicrob Agents Chemother       Date:  2012-08-06       Impact factor: 5.191

4.  Preclinical characterization of the novel hepatitis C virus NS3 protease inhibitor GS-9451.

Authors:  Huiling Yang; Margaret Robinson; Amoreena C Corsa; Betty Peng; Guofeng Cheng; Yang Tian; Yujin Wang; Rowchanak Pakdaman; Marian Shen; Xiaoping Qi; Hongmei Mo; Chin Tay; Steve Krawczyk; X Christopher Sheng; Choung U Kim; Chris Yang; William E Delaney
Journal:  Antimicrob Agents Chemother       Date:  2013-08-12       Impact factor: 5.191

Review 5.  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

6.  Characterization of Hepatitis C virus resistance from a multiple-dose clinical trial of the novel NS5A inhibitor GS-5885.

Authors:  Kelly A Wong; Angela Worth; Ross Martin; Evguenia Svarovskaia; Diana M Brainard; Eric Lawitz; Michael D Miller; Hongmei Mo
Journal:  Antimicrob Agents Chemother       Date:  2013-07-22       Impact factor: 5.191

7.  Preclinical characterization of GS-9669, a thumb site II inhibitor of the hepatitis C virus NS5B polymerase.

Authors:  Martijn Fenaux; Stacey Eng; Stephanie A Leavitt; Yu-Jen Lee; Eric M Mabery; Yang Tian; Daniel Byun; Eda Canales; Michael O Clarke; Edward Doerffler; Scott E Lazerwith; Willard Lew; Qi Liu; Michael Mertzman; Philip Morganelli; Lianhong Xu; Hong Ye; Jennifer Zhang; Mike Matles; Bernard P Murray; Judy Mwangi; Jingyu Zhang; Ahmad Hashash; Steve H Krawczyk; Alison M Bidgood; Todd C Appleby; William J Watkins
Journal:  Antimicrob Agents Chemother       Date:  2012-11-26       Impact factor: 5.938

8.  Avoiding Drug Resistance by Substrate Envelope-Guided Design: Toward Potent and Robust HCV NS3/4A Protease Inhibitors.

Authors:  Ashley N Matthew; Jacqueto Zephyr; Desaboini Nageswara Rao; Mina Henes; Wasih Kamran; Klajdi Kosovrasti; Adam K Hedger; Gordon J Lockbaum; Jennifer Timm; Akbar Ali; Nese Kurt Yilmaz; Celia A Schiffer
Journal:  mBio       Date:  2020-03-31       Impact factor: 7.867

  8 in total

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