Literature DB >> 19201606

Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

Hao Zhang1, Denis E Ryono, Pratik Devasthale, Wei Wang, Kevin O'Malley, Dennis Farrelly, Liqun Gu, Thomas Harrity, Michael Cap, Cuixia Chu, Kenneth Locke, Litao Zhang, Jonathan Lippy, Lori Kunselman, Nathan Morgan, Neil Flynn, Lisa Moore, Vinayak Hosagrahara, Lisa Zhang, Pathanjali Kadiyala, Carrie Xu, Arthur M Doweyko, Aneka Bell, Chiehying Chang, Jodi Muckelbauer, Robert Zahler, Narayanan Hariharan, Peter T W Cheng.   

Abstract

The design, synthesis and structure-activity relationships of a novel series of N-phenyl-substituted pyrrole, 1,2-pyrazole and 1,2,3-triazole acid analogs as PPAR ligands are outlined. The triazole acid analogs 3f and 4f were identified as potent dual PPARalpha/gamma agonists both in binding and functional assays in vitro. The 3-oxybenzyl triazole acetic acid analog 3f showed excellent glucose and triglyceride lowering in diabetic db/db mice.

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Year:  2009        PMID: 19201606     DOI: 10.1016/j.bmcl.2009.01.030

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


  4 in total

Review 1.  Growing applications of "click chemistry" for bioconjugation in contemporary biomedical research.

Authors:  Kido Nwe; Martin W Brechbiel
Journal:  Cancer Biother Radiopharm       Date:  2009-06       Impact factor: 3.099

2.  Molecular modelling study of the PPARγ receptor in relation to the mode of action/adverse outcome pathway framework for liver steatosis.

Authors:  Ivanka Tsakovska; Merilin Al Sharif; Petko Alov; Antonia Diukendjieva; Elena Fioravanzo; Mark T D Cronin; Ilza Pajeva
Journal:  Int J Mol Sci       Date:  2014-05-05       Impact factor: 5.923

3.  Virtual Screening as a Technique for PPAR Modulator Discovery.

Authors:  Stephanie N Lewis; Josep Bassaganya-Riera; David R Bevan
Journal:  PPAR Res       Date:  2009-09-02       Impact factor: 4.964

4.  Molecular recognition of agonist and antagonist for peroxisome proliferator-activated receptor-α studied by molecular dynamics simulations.

Authors:  Mengyuan Liu; Lushan Wang; Xian Zhao; Xun Sun
Journal:  Int J Mol Sci       Date:  2014-05-15       Impact factor: 5.923

  4 in total

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