Literature DB >> 15863293

Selective PPARgamma modulators with improved pharmacological profiles.

Kun Liu1, Regina M Black, John J Acton, Ralph Mosley, Sheryl Debenham, Ramon Abola, Meng Yang, Richard Tschirret-Guth, Lawrence Colwell, Cherrie Liu, Margaret Wu, Chuanlin F Wang, Karen L MacNaul, Margaret E McCann, David E Moller, Joel P Berger, Peter T Meinke, A Brian Jones, Harold B Wood.   

Abstract

A series of metabolically robust N-benzyl-indole selective PPARgamma modulators with either a 3-benzoyl or 3-benzisoxazoyl moiety have been identified. In vitro, these compounds are partial agonists and exhibit reduced adipogenesis in human adipocytes. In vivo, these SPPARgammaMs result in potent glucose lowering in db/db mice and attenuate increases in heart weight and brown adipose tissue that is typically observed in rats upon treatment with PPARgamma full agonists.

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Year:  2005        PMID: 15863293     DOI: 10.1016/j.bmcl.2005.03.092

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


  11 in total

1.  Synthesis of 1-(4-trifluoromethoxyphenyl)-2,5-dimethyl-3-(2-R-thiazol-4-yl)-1H-pyrroles via chain heterocyclization.

Authors:  Mykhaylo V Vovk; Oleksandr M Pinchuk; Andrij O Tolmachov; Andrei A Gakh
Journal:  Molecules       Date:  2010-02-23       Impact factor: 4.411

2.  Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.

Authors:  Alice Asteian; Anne-Laure Blayo; Yuanjun He; Marcel Koenig; Youseung Shin; Dana S Kuruvilla; Cesar A Corzo; Michael D Cameron; Li Lin; Claudia Ruiz; Susan Khan; Naresh Kumar; Scott Busby; David P Marciano; Ruben D Garcia-Ordonez; Patrick R Griffin; Theodore M Kamenecka
Journal:  ACS Med Chem Lett       Date:  2015-08-04       Impact factor: 4.345

Review 3.  Peroxisome proliferator-activated receptors and their ligands: entry into the post-glucocorticoid era of skin treatment?

Authors:  Günther Weindl; Monika Schäfer-Korting; Martin Schaller; Hans Christian Korting
Journal:  Drugs       Date:  2005       Impact factor: 9.546

4.  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

5.  Chemical Crosslinking Mass Spectrometry Reveals the Conformational Landscape of the Activation Helix of PPARγ; a Model for Ligand-Dependent Antagonism.

Authors:  Jie Zheng; Cesar Corzo; Mi Ra Chang; Jinsai Shang; Vinh Q Lam; Richard Brust; Anne-Laure Blayo; John B Bruning; Theodore M Kamenecka; Douglas J Kojetin; Patrick R Griffin
Journal:  Structure       Date:  2018-08-23       Impact factor: 5.006

6.  Peroxisome proliferator-activated receptor gamma-dependent activity of indole ring-substituted 1,1-bis(3'-indolyl)-1-(p-biphenyl)methanes in cancer cells.

Authors:  Jingjing Guo; Sudhakar Chintharlapalli; Syng-ook Lee; Sung Dae Cho; Ping Lei; Sabitha Papineni; Stephen Safe
Journal:  Cancer Chemother Pharmacol       Date:  2009-10-13       Impact factor: 3.333

Review 7.  Benzisoxazole: a privileged scaffold for medicinal chemistry.

Authors:  K P Rakesh; C S Shantharam; M B Sridhara; H M Manukumar; Hua-Li Qin
Journal:  Medchemcomm       Date:  2017-10-31       Impact factor: 3.597

8.  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

9.  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

10.  'Striking the Right Balance' in Targeting PPARgamma in the Metabolic Syndrome: Novel Insights from Human Genetic Studies.

Authors:  Mark Gurnell
Journal:  PPAR Res       Date:  2007       Impact factor: 4.964

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