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Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor gamma/delta agonists

Authors
Gim, Hyo JinLi, HuaJeong, Ji HyeLee, Su JeongSung, Mi-KyungSong, Mi-YoungPark, Byung-HyunOh, Soo JinRyu, Jae-HaJeon, Raok
Issue Date
Jul-2015
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
PPAR; Agonist; Indolylacetic acid; Metabolic disease
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.23, no.13, pp 3322 - 3336
Pages
15
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
Volume
23
Number
13
Start Page
3322
End Page
3336
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/10492
DOI
10.1016/j.bmc.2015.04.046
ISSN
0968-0896
1464-3391
Abstract
A series of alkoxy-3-indolylacetic acid analogs has been discovered as peroxisome proliferator-activated receptor (PPAR) agonists. Structure-activity relationship study indicated that PPAR alpha/gamma/delta activities were dependent on the nature of the hydrophobic group, the attachment position of the alkoxy linker to the indole ring, and N-alkylation of indole nitrogen. Some compounds presented significant PPAR gamma/delta activity and molecular modeling suggested their putative binding modes in the ligand binding domain of PPAR gamma. Of these, compound 51 was selected for in vivo study via an evaluation of microsomal stability in mouse and human liver. Compound 51 lowered the levels of fasting blood glucose, insulin, and HbA1c without gain in body weight in db/db mice. When compound 51 was treated, hepatic triglycerides level and the size of adipocytes in white adipose tissue of db/db mice were also reduced as opposed to treatment with rosiglitazone. Taken together, compound 51 shows high potential warranting further studies in models for diabetes and related metabolic disorders and may be in use as a chemical tool for the understanding of PPAR biology. (C) 2015 Elsevier Ltd. All rights reserved.
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