Literature DB >> 16153845

Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.

James F Dropinski1, Taro Akiyama, Monica Einstein, Bahanu Habulihaz, Tom Doebber, Joel P Berger, Peter T Meinke, Guo Q Shi.   

Abstract

A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARgamma modulators. Their chemical synthesis and in vitro activities are discussed. Compound 5 was selected for in vivo testing in the db/db mouse model of type 2 diabetes and resulted in reduction of hyperglycemia at comparable plasma exposure when compared to rosiglitazone.

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Year:  2005        PMID: 16153845     DOI: 10.1016/j.bmcl.2005.08.002

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


  4 in total

1.  Structural insights for the design of new PPARgamma partial agonists with high binding affinity and low transactivation activity.

Authors:  Laura Guasch; Esther Sala; Cristina Valls; Mayte Blay; Miquel Mulero; Lluís Arola; Gerard Pujadas; Santiago Garcia-Vallvé
Journal:  J Comput Aided Mol Des       Date:  2011-06-21       Impact factor: 3.686

Review 2.  PPARgamma and its ligands: therapeutic implications in cardiovascular disease.

Authors:  Luis Villacorta; Francisco J Schopfer; Jifeng Zhang; Bruce A Freeman; Y Eugene Chen
Journal:  Clin Sci (Lond)       Date:  2009-02       Impact factor: 6.124

3.  Selective Modulators of PPAR-gamma Activity: Molecular Aspects Related to Obesity and Side-Effects.

Authors:  Fang Zhang; Brian E Lavan; Francine M Gregoire
Journal:  PPAR Res       Date:  2007       Impact factor: 4.964

Review 4.  New Insights into the PPAR γ Agonists for the Treatment of Diabetic Nephropathy.

Authors:  Zhanjun Jia; Ying Sun; Guangrui Yang; Aihua Zhang; Songming Huang; Kristina Marie Heiney; Yue Zhang
Journal:  PPAR Res       Date:  2014-01-29       Impact factor: 4.964

  4 in total

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