國家衛生研究院 NHRI:Item 3990099045/1250
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    題名: 3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes
    作者: Coumar, MS;Chang, CN;Chen, CT;Chen, X;Chien, CH;Tsai, TY;Cheng, JH;Wu, HY;Han, CH;Wu, SH;Huang, YW;Hsu, T;Hsu, LJ;Chao, YS;Hsieh, HP;Jiaang, WT
    貢獻者: Division of Biotechnology and Pharmaceutical Research
    摘要: Based on the structures of NVP-DPP728 (1) and NVP-LAF237 (Vildagliptin, 2), three series of DPP-IV inhibitors were synthesized by linking substituted anilines, benzylamines, and phenylethylamines to (2S)-cyanopyrrolidine through a linker. More than 20 compounds were evaluated for their in vitro DPP-IV inhibition and selectivity profile over DPP-II, DPP8, and FAP enzymes. Selected compounds 5f and 7i showed in vivo plasma DPP-IV inhibition and inhibited glucose excursion in OGTT after oral administration in Wistar rats. Compound 5f (DPP-1V IC50 = 116 nM) has the potential for development as antidiabetic agent. (c) 2006 Elsevier Ltd. All rights reserved.
    關鍵詞: Chemistry, Medicinal;Chemistry, Organic
    日期: 2007-03-01
    關聯: Bioorganic and Medicinal Chemistry Letters. 2007 Mar;17(5):1274-1279.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2006.12.019
    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:000244943300028
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=33846986803
    顯示於類別:[蔣維棠] 期刊論文
    [謝興邦] 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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