Literature DB >> 20457518

Discovery of TRPV1 antagonist ABT-116.

Brian S Brown1, Ryan Keddy, Richard J Perner, Stanley DiDomenico, John R Koenig, Tammie K Jinkerson, Steven M Hannick, Heath A McDonald, Bruce R Bianchi, Prisca Honore, Pamela S Puttfarcken, Robert B Moreland, Kennan C Marsh, Connie R Faltynek, Chih-Hung Lee.   

Abstract

The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described. Biological studies demonstrated potent in vitro and in vivo activity for 21, as well as suitable physicochemical and pharmacokinetic properties for advancement to clinical development for pain management. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20457518     DOI: 10.1016/j.bmcl.2010.04.047

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


  5 in total

1.  TRPV1-Targeted Drugs in Development for Human Pain Conditions.

Authors:  Mircea Iftinca; Manon Defaye; Christophe Altier
Journal:  Drugs       Date:  2021-01       Impact factor: 9.546

2.  3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E/eIF4G interaction.

Authors:  Revital Yefidoff-Freedman; Ting Chen; Rupam Sahoo; Limo Chen; Gerhard Wagner; Jose A Halperin; Bertal H Aktas; Michael Chorev
Journal:  Chembiochem       Date:  2014-01-23       Impact factor: 3.164

3.  How Far Could We Go with Open Data - A Case Study for TRPV1 Antagonists.

Authors:  Daria A Tsareva; Gerhard F Ecker
Journal:  Mol Inform       Date:  2013-06-18       Impact factor: 4.050

4.  Effect of analgesic therapy on clinical outcome measures in a randomized controlled trial using client-owned dogs with hip osteoarthritis.

Authors:  Sarah Malek; Susannah J Sample; Zeev Schwartz; Brett Nemke; Peer B Jacobson; Elizabeth M Cozzi; Susan L Schaefer; Jason A Bleedorn; Gerianne Holzman; Peter Muir
Journal:  BMC Vet Res       Date:  2012-10-04       Impact factor: 2.741

5.  Novel scaffolds for modulation of TRPV1 identified with pharmacophore modeling and virtual screening.

Authors:  Daria Goldmann; Peter Pakfeifer; Steffen Hering; Gerhard F Ecker
Journal:  Future Med Chem       Date:  2015       Impact factor: 4.767

  5 in total

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