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
- 탁정애
- Keywords
- Anti-obesity; GW501516; Marine natural products; Nuclear receptors; PPARδ
- Issue Date
- 2012-03
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 23 RUE LINOIS, 75724 PARIS, FRANCE
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 권: 53 페이지: 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.
- URI
- https://www.sciencedirect.com/science/article/pii/S0223523412002176?via%3Dihub
- ISSN
- 0223-5234
- DOI
- 10.1016/j.ejmech.2012.03.055
- Appears in Collections:
- CENTER FOR CREATIVE CONVERGENCE EDUCATION[S](창의융합교육원) > ETC
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