Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor delta agonists as potent anti-obesity agents in vivo
- Authors
- Ham, Jungyeob; Hwang, Hoosang; Kim, Euno; Kim, Jeong-ah; Cho, Sung Jin; Ko, Jaeyoung; Lee, Woojin; Lee, Jaehwan; Holla, Harish; Tak, Jun gae
- Issue Date
- Mar-2012
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- Anti-obesity; GW501516; Marine natural products; Nuclear receptors; PPARδ
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.53, pp.190 - 202
- Indexed
- SCIE
SCOPUS
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 53
- Start Page
- 190
- End Page
- 202
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/166017
- DOI
- 10.1016/j.ejmech.2012.03.055
- ISSN
- 0223-5234
- 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.
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