Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376045 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
A series of potent amide linked PPARγ/δ dual agonists (1a) has been discovered through rational design. In the ZDF rat model of type 2 diabetes, compound (R)-3-[4-(3-{1-[(5-chloro-1,3-dimethyl-1H-indole-2-carbonyl)-amino]-ethyl}-5-fluoro-phenoxy)-2-ethyl-phenyl]-propionic acid (42) from this series has demonstrated glucose lowering efficacy comparable to the marketed PPARγ agonist rosiglitazone with less weight gain.
Graphical abstractThe synthesis and preclinical biological evaluation of a novel amide linked series of PPARγ/δ dual agonists are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Qing Shi, Emily J. Canada, Yanping Xu, Alan M. Warshawsky, Garret J. Etgen, Carol L. Broderick, Cathleen K. Clutinger, Lynnie A. Irwin, Michael E. Laurila, Chahrzad Montrose-Rafizadeh, Brian A. Oldham, Minmin Wang, Leonard L. Winneroski, Chaoyu Xie,