Design and Structural Analysis of Novel Pharmacophores for Potent and Selective Peroxisome Proliferator-activated Receptor gamma Agonists

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dc.citation.epage2622en_US
dc.citation.issue8en_US
dc.citation.spage2618en_US
dc.citation.volume52en_US
dc.citation.woscount8
dc.contributor.authorLin, Chia-Huien_US
dc.contributor.authorPeng, Yi-Huien_US
dc.contributor.authorCoumar, Mohane Selvarajen_US
dc.contributor.authorChittimalla, Santhosh Kumaren_US
dc.contributor.authorLiao, Chun-Chenen_US
dc.contributor.authorLyn, Ping-Chiangen_US
dc.contributor.authorHuang, Chin-Chiehen_US
dc.contributor.authorLien, Tzu-Wenen_US
dc.contributor.authorLin, Wen-Hsingen_US
dc.contributor.authorHsu, John T. -A.en_US
dc.contributor.authorCheng, Jai-Hongen_US
dc.contributor.authorChen, Xinen_US
dc.contributor.authorWu, Jian-Sungen_US
dc.contributor.authorChao, Yu-Shengen_US
dc.contributor.authorLee, Hwei-Jenen_US
dc.contributor.authorJuo, Chiun-Gungen_US
dc.contributor.authorWu, Su-Yingen_US
dc.contributor.authorHsieh, Hsing-Pangen_US
dc.contributor.department生物科技學系zh_TW
dc.contributor.departmentDepartment of Biological Science and Technologyen_US
dc.date.accessioned2014-12-08T15:09:36Z
dc.date.available2014-12-08T15:09:36Z
dc.date.issued2009-04-23en_US
dc.description.abstractUtilizing medicinal chemistry design strategies Such as benzo splitting and ring expansion, we converted PPAR alpha/gamma dual agonist 1 to selective PPAR gamma agonists 19 and 20. Compounds 19 and 20 were 2- to 4-fold better than rosiglitazone at PPAR gamma receptor. with 80- to 100-fold PPAR gamma selectivity over PPAR alpha receptor. X-ray cocrystal studies in PPAR gamma and modeling studies in PPAR alpha give molecular insights for the improved PPAR gamma potency and selectivity for 19 when compared to 1.en_US
dc.identifier.doi10.1021/jm801594xen_US
dc.identifier.issn0022-2623en_US
dc.identifier.journalJOURNAL OF MEDICINAL CHEMISTRYen_US
dc.identifier.urihttp://dx.doi.org/10.1021/jm801594xen_US
dc.identifier.urihttps://ir.lib.nycu.edu.tw/handle/11536/7344
dc.identifier.wosnumberWOS:000265292700044
dc.language.isoen_USen_US
dc.titleDesign and Structural Analysis of Novel Pharmacophores for Potent and Selective Peroxisome Proliferator-activated Receptor gamma Agonistsen_US
dc.typeArticleen_US

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