Design and synthesis of alkoxyindolyl-3-acetic acid analogs as peroxisome proliferator-activated receptor-gamma/delta agonists
- Authors
- Gim, Hyo Jin; Li, Hua; Lee, Eun; Ryu, Jae-Ha; Jeon, Raok
- Issue Date
- 15-Jan-2013
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.23, no.2, pp 513 - 517
- Pages
- 5
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 23
- Number
- 2
- Start Page
- 513
- End Page
- 517
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/11371
- DOI
- 10.1016/j.bmcl.2012.11.033
- ISSN
- 0960-894X
1464-3405
- Abstract
- 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.
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