Literature DB >> 24900232

Pyridine Carboxamides: Potent Palm Site Inhibitors of HCV NS5B Polymerase.

Cliff C Cheng1, Xiaohua Huang1, Gerald W Shipps1, Yu-Sen Wang1, Daniel F Wyss1, Kyle A Soucy1, Chuan-Kui Jiang2, Sony Agrawal2, Eric Ferrari2, Zhiqing He2, H-C Huang2.   

Abstract

Pyridine carboxamide-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified and optimized to a variety of topologically related scaffolds. In particular, the 2-methyl nicotinic acid scaffold was developed into inhibitors with improved biochemical (IC50-GT1b = 0.014 μM) and cell-based HCV replicon potency (EC50-GT1b = 0.7 μM). Biophysical and biochemical characterization identified this novel series of compounds as palm site binders to HCV polymerase.

Entities:  

Keywords:  2D 15N-HSQC; HCV NS5B polymerase; Hepatitis C virus; automated ligand identification system (ALIS); direct-acting antiviral (DAA); palm site inhibitors

Year:  2010        PMID： 24900232      PMCID： PMC4007899          DOI： 10.1021/ml100128h

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  20 in total

Review 1.  Overview of hepatitis C virus genome structure, polyprotein processing, and protein properties.

Authors:  K E Reed; C M Rice
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Review 3.  Review article: specifically targeted anti-viral therapy for hepatitis C - a new era in therapy.

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Review 4.  Global epidemiology of hepatitis C virus infection.

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Journal:  Lancet Infect Dis       Date:  2005-09       Impact factor: 25.071

5.  In vitro resistance study of AG-021541, a novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase.

Authors:  Stephanie T Shi; Koleen J Herlihy; Joanne P Graham; Shella A Fuhrman; Chau Doan; Hans Parge; Michael Hickey; Jingjin Gao; Xiu Yu; Fannie Chau; Javier Gonzalez; Hui Li; Cristina Lewis; Amy K Patick; Rohit Duggal
Journal:  Antimicrob Agents Chemother       Date:  2007-12-10       Impact factor: 5.191

6.  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

7.  Slow binding inhibition and mechanism of resistance of non-nucleoside polymerase inhibitors of hepatitis C virus.

Authors:  Julie Qi Hang; Yanli Yang; Seth F Harris; Vincent Leveque; Hannah J Whittington; Sonal Rajyaguru; Gloria Ao-Ieong; Matthew F McCown; April Wong; Anthony M Giannetti; Sophie Le Pogam; Francisco Talamás; Nick Cammack; Isabel Nájera; Klaus Klumpp
Journal:  J Biol Chem       Date:  2009-02-26       Impact factor: 5.157

8.  Inhibitors of hepatitis C virus polymerase: synthesis and characterization of novel 2-oxy-6-fluoro-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-benzamides.

Authors:  Cliff C Cheng; Gerald W Shipps; Zhiwei Yang; Noriyuki Kawahata; Charles A Lesburg; José S Duca; Jamie Bandouveres; Jack D Bracken; Chuan-kui Jiang; Sony Agrawal; Eric Ferrari; H-C Huang
Journal:  Bioorg Med Chem Lett       Date:  2010-02-18       Impact factor: 2.823

9.  Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line.

Authors:  V Lohmann; F Körner; J Koch; U Herian; L Theilmann; R Bartenschlager
Journal:  Science       Date:  1999-07-02       Impact factor: 47.728

10.  Molecular mechanism of hepatitis C virus replicon variants with reduced susceptibility to a benzofuran inhibitor, HCV-796.

Authors:  Anita Y M Howe; Huiming Cheng; Stephen Johann; Stanley Mullen; Srinivas K Chunduru; Dorothy C Young; Joel Bard; Rajiv Chopra; Girija Krishnamurthy; Tarek Mansour; John O'Connell
Journal:  Antimicrob Agents Chemother       Date:  2008-06-16       Impact factor: 5.191
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  4 in total

1.  Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.

Authors:  Xiaohua Huang; Cliff C Cheng; Thierry O Fischmann; José S Duca; Xianshu Yang; Matthew Richards; Gerald W Shipps
Journal:  ACS Med Chem Lett       Date:  2012-01-20       Impact factor: 4.345

2.  Synthesis and Anti-HCV Activity of 4-Hydroxyamino α-Pyranone Carboxamide Analogues.

Authors:  Ananda Kumar Konreddy; Massaki Toyama; Wataru Ito; Chandralata Bal; Masanori Baba; Ashoke Sharon
Journal:  ACS Med Chem Lett       Date:  2013-12-03       Impact factor: 4.345

3.  Dual Allosteric Inhibitors Jointly Modulate Protein Structure and Dynamics in the Hepatitis C Virus Polymerase.

Authors:  Jodian A Brown; Ian F Thorpe
Journal:  Biochemistry       Date:  2015-06-26       Impact factor: 3.162

4.  Synthesis of Chitosan-La2O3 Nanocomposite and Its Utility as a Powerful Catalyst in the Synthesis of Pyridines and Pyrazoles.

Authors:  Khaled D Khalil; Sayed M Riyadh; Mariusz Jaremko; Thoraya A Farghaly; Mohamed Hagar
Journal:  Molecules       Date:  2021-06-17       Impact factor: 4.411
  4 in total

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