Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor delta agonists as potent anti-obesity agents in vivo

Title
Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor delta agonists as potent anti-obesity agents in vivo
Author(s)
최혁재Jungyeob Ham[Jungyeob Ham]Hoosang Hwang[Hoosang Hwang]Euno Kim[Euno Kim]Jeong-ah Kim[Jeong-ah Kim]Sung Jin Cho[Sung Jin Cho]Jaeyoung Ko[Jaeyoung Ko]Woojin Lee[Woojin Lee]Jaehwan Lee[Jaehwan Lee]Harish Holla[Harish Holla]Joydeep Banerjee[Joydeep Banerjee]Sukho Kim[Sukho Kim]Inho Yang[Inho Yang]Hyun Joo Lee[Hyun Joo Lee]Kyoungjin Shin[Kyoungjin Shin]Sang-Jip Nam[Sang-Jip Nam]Jungae Tak[Jungae Tak]Dongyup Hahn[Dongyup Hahn]Taekyung Oh[Taekyung Oh]Dong Hwan Won[Dong Hwan Won]Tae Gu Lee[Tae Gu Lee]Jihye Choi[Jihye Choi]Mi Sun Park[Mi Sun Park]Chaok Seok[Chaok Seok]Jungwook Chin[Jungwook Chin]Heonjoong Kang[Heonjoong Kang]
Keywords
BETA-OXIDATION PATHWAY; PPAR-DELTA; FATTY-ACIDS; ALPHA; GAMMA; IDENTIFICATION; METABOLISM; EXPRESSION; SULFIDES; LIGANDS
Issue Date
201207
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.53, pp.190 - 202
Abstract
We have discovered and demonstrated the in vitro and in vivo PPAR delta-selective activity of novel Y-shaped agonists. These compounds activated hPPAR delta with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPAR delta agonists with 10(4)-fold selectivity over the other two subtypes, namely, hPPAR alpha and hPPAR gamma. The PPAR delta ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy. (C) 2012 Elsevier Masson SAS. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/27628http://dx.doi.org/10.1016/j.ejmech.2012.03.055
ISSN
0223-5234
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약학대학 > 약학부 > Articles
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