Literature DB >> 15743173

Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.

Steven Harper1, Barbara Pacini, Salvatore Avolio, Marcello Di Filippo, Giovanni Migliaccio, Ralph Laufer, Raffaele De Francesco, Michael Rowley, Frank Narjes.   

Abstract

Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here a novel class of allosteric inhibitor of NS5B that shows potent affinity for the NS5B enzyme and effective inhibition of subgenomic HCV RNA replication in HUH-7 cells. Inhibitors from this class have promising characteristics for further development as anti-HCV agents.

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Year:  2005        PMID: 15743173     DOI: 10.1021/jm049122i

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  13 in total

1.  Discovery of naturally occurring aurones that are potent allosteric inhibitors of hepatitis C virus RNA-dependent RNA polymerase.

Authors:  Romain Haudecoeur; Abdelhakim Ahmed-Belkacem; Wei Yi; Antoine Fortuné; Rozenn Brillet; Catherine Belle; Edwige Nicolle; Coralie Pallier; Jean-Michel Pawlotsky; Ahcène Boumendjel
Journal:  J Med Chem       Date:  2011-07-06       Impact factor: 7.446

2.  An Efficient, Microwave-Assisted, One-Pot Synthesis of Indoles Under Sonogashira Conditions.

Authors:  Yu Chen; Nataliya A Markina; Richard C Larock
Journal:  Tetrahedron       Date:  2009-10-31       Impact factor: 2.457

3.  Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees.

Authors:  Steven S Carroll; Steven Ludmerer; Larry Handt; Kenneth Koeplinger; Nanyan Rena Zhang; Donald Graham; Mary-Ellen Davies; Malcolm MacCoss; Daria Hazuda; David B Olsen
Journal:  Antimicrob Agents Chemother       Date:  2008-12-15       Impact factor: 5.191

4.  Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation.

Authors:  Jiaojiao Li; Jing Ji; Ruibo Xu; Zhengfu Li
Journal:  Medchemcomm       Date:  2019-09-17       Impact factor: 3.597

5.  Binding-site identification and genotypic profiling of hepatitis C virus polymerase inhibitors.

Authors:  Frederik Pauwels; Wendy Mostmans; Ludo M M Quirynen; Liesbet van der Helm; Carlo W Boutton; Anne-Stéphanie Rueff; Erna Cleiren; Pierre Raboisson; Dominique Surleraux; Origène Nyanguile; Kenneth A Simmen
Journal:  J Virol       Date:  2007-04-25       Impact factor: 5.103

6.  Novel indole-2-carboxamide compounds are potent broad-spectrum antivirals active against western equine encephalitis virus in vivo.

Authors:  Phillip C Delekta; Craig J Dobry; Janice A Sindac; Scott J Barraza; Pennelope K Blakely; Jianming Xiang; Paul D Kirchhoff; Richard F Keep; David N Irani; Scott D Larsen; David J Miller
Journal:  J Virol       Date:  2014-07-16       Impact factor: 5.103

7.  Discovery and characterization of substituted diphenyl heterocyclic compounds as potent and selective inhibitors of hepatitis C virus replication.

Authors:  Peiyong Huang; Dane A Goff; Qi Huang; Anthony Martinez; Xiang Xu; Scott Crowder; Sarkiz D Issakani; Emily Anderson; Ning Sheng; Philip Achacoso; Ann Yen; Todd Kinsella; Ihab S Darwish; Rao Kolluri; Hui Hong; Kunbin Qu; Emily Stauffer; Eileen Goldstein; Rajinder Singh; Donald G Payan; H Henry Lu
Journal:  Antimicrob Agents Chemother       Date:  2008-01-28       Impact factor: 5.191

8.  TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage.

Authors:  Benoit Devogelaere; Jan Martin Berke; Leen Vijgen; Pascale Dehertogh; Els Fransen; Erna Cleiren; Liesbet van der Helm; Origène Nyanguile; Abdellah Tahri; Katie Amssoms; Oliver Lenz; Maxwell D Cummings; Reginald F Clayton; Sandrine Vendeville; Pierre Raboisson; Kenneth A Simmen; Gregory C Fanning; Tse-I Lin
Journal:  Antimicrob Agents Chemother       Date:  2012-06-18       Impact factor: 5.191

9.  Practical synthesis of indoles and benzofurans in water using a heterogeneous bimetallic catalyst.

Authors:  Cybille Rossy; Eric Fouquet; François-Xavier Felpin
Journal:  Beilstein J Org Chem       Date:  2013-07-16       Impact factor: 2.883

10.  Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) of thiazolone derivatives as hepatitis C virus NS5B polymerase allosteric inhibitors.

Authors:  Beilei Lei; Juan Du; Shuyan Li; Huanxiang Liu; Yueying Ren; Xiaojun Yao
Journal:  J Comput Aided Mol Des       Date:  2008-08-21       Impact factor: 3.686

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