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

Authors
Henke, BR Adkison, KK Blanchard, SG Leesnitzer, LM Mook, RA Plunket, KD Ray, JA Roberson, C Unwalla, R Willson, TM
Citation
Br. Henke et al., Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists, BIOORG MED, 9(23), 1999, pp. 3329-3334
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
23
Year of publication
1999
Pages
3329 - 3334
Database
ISI
SICI code
0960-894X(199912)9:23<3329:SABAOA>2.0.ZU;2-H
Abstract
The synthesis and structure-activity relationships of a novel series of ind ole 5-carboxylic acids that bind and activate peroxisome proliferator-activ ated receptor gamma (PPAR gamma) are reported. These new analogs are select ive for PPAR gamma vs the other PPAR subtypes, and the most potent compound s in this series are comparable to in vitro potencies at PPAR gamma reporte d for the thiazolidinedione-based antidiabetic drugs currently in clinical use. (C) 1999 Elsevier Science Ltd. All rights reserved.