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Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-gamma/delta dual agonists

Authors
Gim, Hyo JinCheon, Ye-JinRyu, Jae-HaJeon, Raok
Issue Date
15-May-2011
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Indole; Benzoxazole; PPAR; Diabetes
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.21, no.10, pp 3057 - 3061
Pages
5
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
21
Number
10
Start Page
3057
End Page
3061
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/12572
DOI
10.1016/j.bmcl.2011.03.027
ISSN
0960-894X
1464-3405
Abstract
A series of benzoxazole or benzothiazole containing indole analogs, 6-alkoxyindole-2-carboxylic acids and 5-alkoxy-3-indolylacetic acids, were synthesized as novel candidates of PPAR gamma/delta dual agonists and their ligand activities for PPAR subtypes (alpha, gamma and delta) were investigated. In transient transactivation assay, several compounds activated PPAR gamma and delta with little activity of PPAR alpha. Putative binding mode of the compounds 1a and 2a in the active site of PPAR gamma was similar with that of rosiglitazone and the molecular modeling provides molecular insight to the observed activity. (C) 2011 Elsevier Ltd. All rights reserved.
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