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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
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18초록
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-DELTA; ROSIGLITAZONE; TARGET; LIGAND; GAMMA; DEATH
- 제목
- Design and synthesis of alkoxyindolyl-3-acetic acid analogs as peroxisome proliferator-activated receptor-gamma/delta agonists
- 저자
- Gim, Hyo Jin; Li, Hua; Lee, Eun; Ryu, Jae-Ha; Jeon, Raok
- 발행일
- 2013-01-15
- 유형
- Article
- 권
- 23
- 호
- 2
- 페이지
- 513 ~ 517