Literature DB >> 21414782

Phenoxyacetic acids as PPARδ partial agonists: synthesis, optimization, and in vivo efficacy.

Karen A Evans1, Barry G Shearer, David D Wisnoski, Dongchuan Shi, Steven M Sparks, Daniel D Sternbach, Deborah A Winegar, Andrew N Billin, Christy Britt, James M Way, Andrea H Epperly, Lisa M Leesnitzer, Raymond V Merrihew, Robert X Xu, Millard H Lambert, Jian Jin.   

Abstract

A series of phenoxyacetic acids as subtype selective and potent hPPARδ partial agonists is described. Many analogues were readily accessible via a single solution-phase synthetic route which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of two potent exemplars which were further evaluated in vivo. Details of the SAR, optimization, and in vivo efficacy of this series are presented herein.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21414782     DOI: 10.1016/j.bmcl.2011.02.077

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


  2 in total

Review 1.  Activation of PPARδ: from computer modelling to biological effects.

Authors:  Shirin Kahremany; Ariela Livne; Arie Gruzman; Hanoch Senderowitz; Shlomo Sasson
Journal:  Br J Pharmacol       Date:  2014-12-15       Impact factor: 8.739

2.  Structure-based virtual screening and discovery of New PPARδ/γ dual agonist and PPARδ and γ agonists.

Authors:  Vinicius G Maltarollo; Marie Togashi; Alessandro S Nascimento; Kathia M Honorio
Journal:  PLoS One       Date:  2015-03-13       Impact factor: 3.240

  2 in total

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