Literature DB >> 23466233

Synthesis and evaluation of non-dimeric HCV NS5A inhibitors.

Franck Amblard1, 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.   

Abstract

Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000).
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23466233      PMCID： PMC3602317          DOI： 10.1016/j.bmcl.2013.02.023

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


  7 in total

1.  Hepatitis C--global prevalence (update).

Authors: 
Journal:  Wkly Epidemiol Rec       Date:  1999-12-10

2.  NS5A inhibitors: a new breakthrough for the treatment of chronic hepatitis C.

Authors:  Tarik Asselah
Journal:  J Hepatol       Date:  2010-12-16       Impact factor: 25.083

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

Review 4.  Treatment of hepatitis C.

Authors:  Andrew I Kim; Sammy Saab
Journal:  Am J Med       Date:  2005-08       Impact factor: 4.965

5.  Synthesis and evaluation of novel potent HCV NS5A inhibitors.

Authors:  Hongwang Zhang; 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
Journal:  Bioorg Med Chem Lett       Date:  2012-05-24       Impact factor: 2.823

Review 6.  Development of novel therapies for hepatitis C.

Authors:  Stanley M Lemon; Jane A McKeating; Thomas Pietschmann; David N Frick; Jeffrey S Glenn; Timothy L Tellinghuisen; Julian Symons; Phillip A Furman
Journal:  Antiviral Res       Date:  2010-04       Impact factor: 5.970

7.  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
  7 in total
  7 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.  2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.

Authors:  Maruti Naik; Sandeep Ghorpade; Lalit Kumar Jena; Gopinath Gorai; Ashwini Narayan; Supreeth Guptha; Sreevalli Sharma; Neela Dinesh; Parvinder Kaur; Radha Nandishaiah; Jyothi Bhat; Gayathri Balakrishnan; Vaishali Humnabadkar; Vasanthi Ramachandran; Lava Kumar Naviri; Pallavi Khadtare; Manoranjan Panda; Pravin S Iyer; Monalisa Chatterji
Journal:  ACS Med Chem Lett       Date:  2014-07-11       Impact factor: 4.345

3.  The crystal structure of NS5A domain 1 from genotype 1a reveals new clues to the mechanism of action for dimeric HCV inhibitors.

Authors:  Sebastian M Lambert; David R Langley; James A Garnett; Richard Angell; Katy Hedgethorne; Nicholas A Meanwell; Steve J Matthews
Journal:  Protein Sci       Date:  2014-04-05       Impact factor: 6.725

4.  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

5.  Sulfur(vi) fluoride exchange as a key reaction for synthesizing biaryl sulfate core derivatives as potent hepatitis C virus NS5A inhibitors and their structure-activity relationship studies.

Authors:  Youngsu You; Hee Sun Kim; Jung Woo Park; Gyochang Keum; Sung Key Jang; B Moon Kim
Journal:  RSC Adv       Date:  2018-09-12       Impact factor: 4.036

6.  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

Review 7.  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
  7 in total

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