國家衛生研究院 NHRI:Item 3990099045/3553
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/3553


    Title: Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
    Authors: Tsai, TY;Hsu, T;Chen, CT;Cheng, JH;Yeh, TK;Chen, X;Huang, CY;Chang, CN;Yeh, KC;Hsieh, SH;Chien, CH;Chang, YW;Huang, CH;Huang, YW;Huang, CL;Wu, SH;Wang, MH;Lu, CT;Chao, YS;Jiaang, WT
    Contributors: Division of Biotechnology and Pharmaceutical Research
    Abstract: A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC50 values of <100 nM with excellent selectivity over the closely related enzymes, DPP8, DPP-II and FAP. The studies identified a potent and selective DPP-IV inhibitor 24b, which exhibited the ability to both significantly inhibit plasma DPP-IV activity in rats and improve glucose tolerance in lean mice and diet induced obese mice.
    Date: 2009-03-15
    Relation: Bioorganic and Medicinal Chemistry. 2009 Mar 15;17(6):2388-2399.
    Link to: http://dx.doi.org/10.1016/j.bmc.2009.02.020
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0968-0896&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000264236700032
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=62549138270
    Appears in Collections:[Weir-Torn Jiaang] Periodical Articles
    [Teng-Kuang Yeh] Periodical Articles
    [Xin Chen(2002-2015)] Periodical Articles
    [Yu-Sheng Chao(2002-2013)] Periodical Articles
    [Chiung-Tong Chen] Periodical Articles

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