Literature DB >> 22704887

Synthesis and evaluation of novel potent HCV NS5A inhibitors.

Hongwang Zhang1, Longhu Zhou, Franck Amblard, Junxing Shi, Drew R Bobeck, Sijia Tao, Tamara R McBrayer, Phillip M Tharnish, Tony Whitaker, Steven J Coats, Raymond F Schinazi.   

Abstract

Judicious modifications to the structure of the previously reported HCV NS5A inhibitor 1, resulted in more potent anti-HCV compounds with similar and in some cases improved toxicity profiles. The synthesis of 19 new NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. For the most potent compounds chemical stability, stability in liver microsomes and inhibition of relevant CYP450 enzymes is also presented.
Copyright © 2012 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2012        PMID： 22704887      PMCID： PMC3389222          DOI： 10.1016/j.bmcl.2012.05.039

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


  10 in total

1.  Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.

Authors:  Suja Shrestha; Bharat Raj Bhattarai; Keun-Hyeung Lee; Hyeongjin Cho
Journal:  Bioorg Med Chem       Date:  2007-07-26       Impact factor: 3.641

Review 2.  Advances in nucleoside monophosphate prodrugs as anti-HCV agents.

Authors:  Drew R Bobeck; Raymond F Schinazi; Steven J Coats
Journal:  Antivir Ther       Date:  2010

3.  New Merck and Vertex drugs raise standard of care in hepatitis C.

Authors:  Cormac Sheridan
Journal:  Nat Biotechnol       Date:  2011-07-11       Impact factor: 54.908

4.  Resistance analysis of the hepatitis C virus NS5A inhibitor BMS-790052 in an in vitro replicon system.

Authors:  Robert A Fridell; Dike Qiu; Chunfu Wang; Lourdes Valera; Min Gao
Journal:  Antimicrob Agents Chemother       Date:  2010-06-28       Impact factor: 5.191

Review 5.  Copper-catalyzed azide-alkyne cycloaddition (CuAAC) and beyond: new reactivity of copper(I) acetylides.

Authors:  Jason E Hein; Valery V Fokin
Journal:  Chem Soc Rev       Date:  2010-03-04       Impact factor: 54.564

Review 6.  Cu(I)-catalyzed Huisgen azide-alkyne 1,3-dipolar cycloaddition reaction in nucleoside, nucleotide, and oligonucleotide chemistry.

Authors:  Franck Amblard; Jong Hyun Cho; Raymond F Schinazi
Journal:  Chem Rev       Date:  2009-09       Impact factor: 60.622

Review 7.  HCV drug discovery aimed at viral eradication.

Authors:  R F Schinazi; L Bassit; C Gavegnano
Journal:  J Viral Hepat       Date:  2009-12-18       Impact factor: 3.728

8.  Ser(2194) is a highly conserved major phosphorylation site of the hepatitis C virus nonstructural protein NS5A.

Authors:  M G Katze; B Kwieciszewski; D R Goodlett; C M Blakely; P Neddermann; S L Tan; R Aebersold
Journal:  Virology       Date:  2000-12-20       Impact factor: 3.616

9.  Identification of hepatitis C virus NS5A inhibitors.

Authors:  Julie A Lemm; Donald O'Boyle; Mengping Liu; Peter T Nower; Richard Colonno; Milind S Deshpande; Lawrence B Snyder; Scott W Martin; Denis R St Laurent; Michael H Serrano-Wu; Jeffrey L Romine; Nicholas A Meanwell; Min Gao
Journal:  J Virol       Date:  2010-01       Impact factor: 5.103

10.  Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect.

Authors:  Min Gao; Richard E Nettles; Makonen Belema; Lawrence B Snyder; Van N Nguyen; Robert A Fridell; Michael H Serrano-Wu; David R Langley; Jin-Hua Sun; Donald R O'Boyle; Julie A Lemm; Chunfu Wang; Jay O Knipe; Caly Chien; Richard J Colonno; Dennis M Grasela; Nicholas A Meanwell; Lawrence G Hamann
Journal:  Nature       Date:  2010-04-21       Impact factor: 49.962
  10 in total
  5 in total

1.  Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.

Authors:  Il Hak Bae; Jin Kyu Choi; Chieyeon Chough; Sun Ju Keum; Heesun Kim; Sung Key Jang; B Moon Kim
Journal:  ACS Med Chem Lett       Date:  2013-12-04       Impact factor: 4.345

2.  Asymmetric binding to NS5A by daclatasvir (BMS-790052) and analogs suggests two novel modes of HCV inhibition.

Authors:  James H Nettles; Richard A Stanton; Joshua Broyde; Franck Amblard; Hongwang Zhang; Longhu Zhou; Junxing Shi; Tamara R McBrayer; Tony Whitaker; Steven J Coats; James J Kohler; Raymond F Schinazi
Journal:  J Med Chem       Date:  2014-11-03       Impact factor: 7.446

3.  Design, synthesis and evaluation of novel anti-HCV molecules that deliver intracellularly three highly potent NS5A inhibitors.

Authors:  Sebastien Boucle; Sijia Tao; Franck Amblard; Richard A Stanton; James H Nettles; Chengwei Li; Tamara R McBrayer; Tony Whitaker; Steven J Coats; Raymond F Schinazi
Journal:  Bioorg Med Chem Lett       Date:  2015-06-15       Impact factor: 2.823

4.  Synthesis and evaluation of non-dimeric HCV NS5A inhibitors.

Authors:  Franck Amblard; Hongwang Zhang; Longhu Zhou; Junxing Shi; Drew R Bobeck; James H Nettles; Satish Chavre; Tamara R McBrayer; Philip Tharnish; Tony Whitaker; Steven J Coats; Raymond F Schinazi
Journal:  Bioorg Med Chem Lett       Date:  2013-02-13       Impact factor: 2.823

Review 5.  Approaches to hepatitis C treatment and cure using NS5A inhibitors.

Authors:  James J Kohler; James H Nettles; Franck Amblard; Selwyn J Hurwitz; Leda Bassit; Richard A Stanton; Maryam Ehteshami; Raymond F Schinazi
Journal:  Infect Drug Resist       Date:  2014-03-05       Impact factor: 4.003
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.