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Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor α and γ dual agonists

Title
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor α and γ dual agonists
Authors
Suh Y.-G.Kim N.-J.Koo B.-W.Lee K.-O.Moon S.-H.Shin D.-H.Jung J.-W.Paek S.-M.Chang D.-J.Li F.Kang H.-J.Le T.V.T.Yu N.C.Chang Y.S.Kim M.-K.Joong I.L.Ryu J.-S.Park H.-J.
Ewha Authors
류재상
SCOPUS Author ID
류재상scopus
Issue Date
2008
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 51, no. 20, pp. 6318 - 6333
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
In an effort to develop dual PPARα/γ activators with improved therapeutic efficacy, a series of diaryl α-ethoxy propanoic acid compounds comprising two aryl groups linked by rigid oxime ether or isoxazoline ring were designed and synthesized and their biological activities were examined. Most of the compounds possessing an oxime ether linker were more potent PPARγ activators than the lead PPARα/γ dual agonist, tesaglitazar in vitro. Compound 18, one of the derivatives with an oxime ether linker, was found to selectively transactivate PPARγ (EC 50 = 0.028 μM) over PPARα (EC 50 = 7.22 μM) in vitro and lower blood glucose in db/db mice more than muraglitazar after oral treatment for 11 days. © 2008 American Chemical Society.
DOI
10.1021/jm8003416
Appears in Collections:
약학대학 > 약학과 > Journal papers
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