國家衛生研究院 NHRI:Item 3990099045/4786
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/4786


    Title: (2S,4S)-1-[2-(1,1-Dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
    Authors: Yeh, TK;Tsai, TY;Hsu, T;Cheng, JH;Chen, X;Song, JS;Shy, HS;Chiou, MC;Chien, CH;Tseng, YJ;Huang, CY;Yeh, KC;Huang, YL;Huang, CH;Huang, YW;Wang, MH;Tang, HK;Chao, YS;Chen, CT;Jiaang, WT
    Contributors: Division of Biotechnology and Pharmaceutical Research
    Abstract: A series of 2-[3-[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-based DPP-IV inhibitors with various monocyclic amines were synthesized. The structure-activity relationships (SAR) led to the discovery of potent DPP-IV inhibitors, having IC50 values of <100 nM with excellent selectivity over the closely related enzymes, DPP-II, DPP8, DPP9 and FAP (IC50 > 20 μM). Of these compounds, the analogues 12a, 12h and 12i exhibited a long-lasting ex vivo DPP-IV inhibition in rats.
    Date: 2010-06-15
    Relation: Bioorganic and Medicinal Chemistry Letters. 2010 Jun 15;20(12):3596-3600.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2010.04.124
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000278208200031
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77954218296
    Appears in Collections:[Xin Chen(2002-2015)] Periodical Articles
    [Teng-Kuang Yeh] Periodical Articles
    [Yu-Sheng Chao(2002-2013)] Periodical Articles
    [Chiung-Tong Chen] Periodical Articles
    [Weir-Torn Jiaang] Periodical Articles

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