國家衛生研究院 NHRI:Item 3990099045/4366
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    題名: (1,3-Diphenyl-1H-pyrazol-4-yl)-methylamine analogues as inhibitors of dipeptidyl peptidases
    作者: Hsu, T;Chen, CT;Tsai, TY;Cheng, JH;Wu, SY;Chang, CN;Chien, CH;Yeh, KC;Huang, YW;Huang, CL;Huang, CY;Wu, SH;Chiang, YK;Wang, MH;Chao, YS;Chen, X;Jiaang, WT
    貢獻者: Division of Biotechnology and Pharmaceutical Research
    摘要: A number of pyrazole compounds reported in literatures elicit anti-hyperglycemic effects. By modifying the side chain of the heterocyclic skeleton, a new chemical class of DPP-IV inhibitors structurally derived from the (pyrazol-4-yl)-methylamine scaffold have been discovered and evaluated the biological activities of these inhibitors against DPP-IV, DPP8, DPP-II and FAP. The SAR studies showed the (1,3-diphenyl-1H-pyrazol-4-yl)-methylamines with 2,4-dichloro substituents at the 3-phenyl ring selectively preferred as DPP-IV inhibitors, whereas with difluoro substituents at the 3-phenyl ring selectively preferred as DPP8 inhibitors. The binding mode of representative compound 15h at the active site of DPP-IV was predicted by computer model. In additional, 15h exhibited the ability to significantly decrease the glucose excursion in mice.
    日期: 2009-10
    關聯: Journal of the Chinese Chemical Society. 2009 Oct;56(5):1048-1055.
    Link to: http://chemistry.org.tw/public_jour_elec.php?flag=available
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0009-4536&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000272985700025
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77952393642
    顯示於類別:[伍素瑩] 期刊論文
    [陳炯東] 期刊論文
    [陳新(2002-2015)] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [蔣維棠] 期刊論文

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