Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-gamma/delta dual agonists
  • Gim, Hyo Jin
  • Cheon, Ye-Jin
  • Ryu, Jae-Ha
  • Jeon, Raok
Citations

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17
Citations

SCOPUS

18

초록

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.

키워드

IndoleBenzoxazolePPARDiabetesGAMMAAGENTS
제목
Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-gamma/delta dual agonists
저자
Gim, Hyo JinCheon, Ye-JinRyu, Jae-HaJeon, Raok
DOI
10.1016/j.bmcl.2011.03.027
발행일
2011-05-15
유형
Article
저널명
Bioorganic and Medicinal Chemistry Letters
21
10
페이지
3057 ~ 3061