Literature DB >> 15006379

Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.

Robert B Perni1, Janos Pitlik, Shawn D Britt, John J Court, Lawrence F Courtney, David D Deininger, Luc J Farmer, Cynthia A Gates, Scott L Harbeson, Rhonda B Levin, Chao Lin, Kai Lin, Young-Choon Moon, Yu-Ping Luong, Ethan T O'Malley, B Govinda Rao, John A Thomson, Roger D Tung, John H Van Drie, Yunyi Wei.   

Abstract

The alpha-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3.4A protease inhibitors. Structure-activity relationships and prime side optimization are discussed.

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Year:  2004        PMID: 15006379     DOI: 10.1016/j.bmcl.2004.01.022

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


  10 in total

1.  Drug resistance against HCV NS3/4A inhibitors is defined by the balance of substrate recognition versus inhibitor binding.

Authors:  Keith P Romano; Akbar Ali; William E Royer; Celia A Schiffer
Journal:  Proc Natl Acad Sci U S A       Date:  2010-11-17       Impact factor: 11.205

2.  Discovery and development of telaprevir: an NS3-4A protease inhibitor for treating genotype 1 chronic hepatitis C virus.

Authors:  Ann D Kwong; Robert S Kauffman; Patricia Hurter; Peter Mueller
Journal:  Nat Biotechnol       Date:  2011-11-08       Impact factor: 54.908

Review 3.  Current and potential treatments for ubiquitous but neglected herpesvirus infections.

Authors:  Jonathan E Gable; Timothy M Acker; Charles S Craik
Journal:  Chem Rev       Date:  2014-10-02       Impact factor: 60.622

4.  Covalent Antiviral Agents.

Authors:  Sako Mirzaie; Fatemeh Abdi; Amin GhavamiNejad; Brian Lu; Xiao Yu Wu
Journal:  Adv Exp Med Biol       Date:  2021       Impact factor: 2.622

5.  Design, structure-based focusing and in silico screening of combinatorial library of peptidomimetic inhibitors of Dengue virus NS2B-NS3 protease.

Authors:  Vladimir Frecer; Stanislav Miertus
Journal:  J Comput Aided Mol Des       Date:  2010-03-21       Impact factor: 3.686

6.  Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease.

Authors:  Robert B Perni; Susan J Almquist; Randal A Byrn; Gurudatt Chandorkar; Pravin R Chaturvedi; Lawrence F Courtney; Caroline J Decker; Kirk Dinehart; Cynthia A Gates; Scott L Harbeson; Angela Heiser; Gururaj Kalkeri; Elaine Kolaczkowski; Kai Lin; Yu-Ping Luong; B Govinda Rao; William P Taylor; John A Thomson; Roger D Tung; Yunyi Wei; Ann D Kwong; Chao Lin
Journal:  Antimicrob Agents Chemother       Date:  2006-03       Impact factor: 5.191

7.  SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells.

Authors:  B A Malcolm; R Liu; F Lahser; S Agrawal; B Belanger; N Butkiewicz; R Chase; F Gheyas; A Hart; D Hesk; P Ingravallo; C Jiang; R Kong; J Lu; J Pichardo; A Prongay; A Skelton; X Tong; S Venkatraman; E Xia; V Girijavallabhan; F G Njoroge
Journal:  Antimicrob Agents Chemother       Date:  2006-03       Impact factor: 5.191

8.  Molecular basis of telaprevir resistance due to V36 and T54 mutations in the NS3-4A protease of the hepatitis C virus.

Authors:  Christoph Welsch; Francisco S Domingues; Simone Susser; Iris Antes; Christoph Hartmann; Gabriele Mayr; Andreas Schlicker; Christoph Sarrazin; Mario Albrecht; Stefan Zeuzem; Thomas Lengauer
Journal:  Genome Biol       Date:  2008-01-23       Impact factor: 13.583

Review 9.  Antiviral Drug Discovery: Norovirus Proteases and Development of Inhibitors.

Authors:  Kyeong-Ok Chang; Yunjeong Kim; Scott Lovell; Athri D Rathnayake; William C Groutas
Journal:  Viruses       Date:  2019-02-25       Impact factor: 5.048

Review 10.  Synthetic approaches and pharmacological activity of 1,3,4-oxadiazoles: a review of the literature from 2000-2012.

Authors:  Cledualdo Soares de Oliveira; Bruno Freitas Lira; José Maria Barbosa-Filho; Jorge Gonçalo Fernandez Lorenzo; Petrônio Filgueiras de Athayde-Filho
Journal:  Molecules       Date:  2012-08-27       Impact factor: 4.411

  10 in total

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