Design and synthesis of alkoxyindolyl-3-acetic acid analogs as peroxisome proliferator-activated receptor-gamma/delta agonists
  • Gim, Hyo Jin
  • Li, Hua
  • Lee, Eun
  • Ryu, Jae-Ha
  • Jeon, Raok
Citations

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15
Citations

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18

초록

A series of carbazole or phenoxazine containing alkoxyindole-3-acetic acid analogs were prepared as PPAR gamma/delta agonists and their transactivation activities for PPAR receptor subtypes (alpha, gamma and delta) were investigated. Structure-activity relationship studies disclosed the effect of the lipophilic tail, attaching position of the alkoxy group and N-benzyl substitution at indole. Compound 1b was the most potent for PPARd and 3b for PPAR gamma. Molecular modeling suggested two different binding modes of our alkoxyindole-3-acetic acid analogs providing the insight into their PPAR activity. (C) 2012 Elsevier Ltd. All rights reserved.

키워드

PPAR-DELTAROSIGLITAZONETARGETLIGANDGAMMADEATH
제목
Design and synthesis of alkoxyindolyl-3-acetic acid analogs as peroxisome proliferator-activated receptor-gamma/delta agonists
저자
Gim, Hyo JinLi, HuaLee, EunRyu, Jae-HaJeon, Raok
DOI
10.1016/j.bmcl.2012.11.033
발행일
2013-01-15
유형
Article
저널명
Bioorganic and Medicinal Chemistry Letters
23
2
페이지
513 ~ 517