國家衛生研究院 NHRI:Item 3990099045/3554
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    题名: Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists
    作者: Lin, CH;Peng, YH;Coumar, MS;Chittimalla, SK;Liao, CC;Lyn, PC;Huang, CC;Lien, TW;Lin, WH;Hsu, JT;Cheng, JH;Chen, X;Wu, JS;Chao, YS;Lee, HJ;Juo, CG;Wu, SY;Hsieh, HP
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: Utilizing medicinal chemistry design strategies such as benzo splitting and ring expansion, we converted PPARα/γ dual agonist 1 to selective PPARα agonists 19 and 20. Compounds 19 and 20 were 2- to 4-fold better than rosiglitazone at PPARγ receptor, with 80- to 100-fold PPARγ selectivity over PPARα receptor. X-ray cocrystal studies in PPARγ and modeling studies in PPARα give molecular insights for the improved PPARγ potency and selectivity for 19 when compared to 1.
    日期: 2009-04-23
    關聯: Journal of Medicinal Chemistry. 2009 Apr 23;52(8):2618-2622.
    Link to: http://dx.doi.org/10.1021/jm801594x
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000265292700044
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=65249083580
    显示于类别:[謝興邦] 期刊論文
    [徐祖安] 期刊論文
    [伍素瑩] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [陳新(2002-2015)] 期刊論文

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