國家衛生研究院 NHRI:Item 3990099045/1256
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    题名: Novel indole-based peroxisome proliferator-activated receptor agonists: Design, SAR, structural biology, and biological activities
    作者: Mahindroo, N;Huang, CF;Peng, YH;Wang, CC;Liao, CC;Lien, TW;Chittimalla, SK;Huang, WJ;Chai, CH;Prakash, E;Chen, CP;Hsu, TA;Peng, CH;Lu, IL;Lee, LH;Chang, YW;Chen, WC;Chou, YC;Chen, CT;Goparaju, CMV;Chen, YS;Lan, SJ;Yu, MC;Chen, X;Chao, YS;Wu, SY;Hsieh, HP
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: The synthesis and structure-activity relationship studies of novel indole derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Indole, a druglike scaffold, was studied as a core skeleton for the acidic head part of PPAR agonists. The structural features (acidic head, substitution on indole, and linker) were optimized first, by keeping benzisoxazole as the tail part, based on binding and functional activity at PPAR gamma protein. The variations in the tail part, by introducing various heteroaromatic ring systems, were then studied. In vitro evaluation led to identification of a novel series of indole compounds with a benzisoxazole tail as potent PPAR agonists with the lead compound 14 (BPR1H036) displaying an excellent pharmacokinetic profile in BALB/c mice and an efficacious glucose lowering activity in KKA(y) mice. Structural biology studies of 14 showed that the indole ring contributes strong hydrophobic interactions with PPAR gamma and could be an important moiety for the binding to the protein.
    关键词: Chemistry, Medicinal
    日期: 2005-12-29
    關聯: Journal of Medicinal Chemistry. 2005 Dec;48(26):8194-8208.
    Link to: http://dx.doi.org/10.1021/jm0506930
    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:000234301800012
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=29744432852
    显示于类别:[謝興邦] 期刊論文
    [伍素瑩] 期刊論文
    [徐祖安] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [陳新(2002-2015)] 期刊論文
    [陳炯東] 期刊論文

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