Literature DB >> 10612594

Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.

B R Henke1, K K Adkison, S G Blanchard, L M Leesnitzer, R A Mook, K D Plunket, J A Ray, C Roberson, R Unwalla, T M Willson.   

Abstract

The synthesis and structure-activity relationships of a novel series of indole 5-carboxylic acids that bind and activate peroxisome proliferator-activated receptor gamma (PPARgamma) are reported. These new analogs are selective for PPARgamma vs the other PPAR subtypes, and the most potent compounds in this series are comparable to in vitro potencies at PPARgamma reported for the thiazolidinedione-based antidiabetic drugs currently in clinical use.

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Year:  1999        PMID: 10612594     DOI: 10.1016/s0960-894x(99)00603-4

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


  4 in total

Review 1.  Peroxisome proliferator-activated receptors.

Authors:  Ouliana Ziouzenkova; Stephane Perrey; Niko Marx; Daniel Bacqueville; Jorge Plutzky
Journal:  Curr Atheroscler Rep       Date:  2002-01       Impact factor: 5.113

2.  3D QSAR studies on peroxisome proliferator-activated receptor gamma agonists using CoMFA and CoMSIA.

Authors:  Chenzhong Liao; Aihua Xie; Jiaju Zhou; Leming Shi; Zhibin Li; Xian-Ping Lu
Journal:  J Mol Model       Date:  2004-03-12       Impact factor: 1.810

3.  A tandem regression-outlier analysis of a ligand cellular system for key structural modifications around ligand binding.

Authors:  Ying-Ting Lin
Journal:  J Cheminform       Date:  2013-04-30       Impact factor: 5.514

4.  Identification of a Novel PPAR-γ Agonist through a Scaffold Tuning Approach.

Authors:  Hyo Jin Gim; Yong-Sung Choi; Hua Li; Yoon-Jung Kim; Jae-Ha Ryu; Raok Jeon
Journal:  Int J Mol Sci       Date:  2018-10-04       Impact factor: 5.923

  4 in total

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