國家衛生研究院 NHRI:Item 3990099045/1248
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    題名: 2-[3-[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
    作者: Tsu, H;Chen, X;Chen, CT;Lee, SJ;Chang, CN;Kao, KH;Coumar, MS;Yeh, YT;Chien, CH;Wang, HS;Lin, KT;Chang, YY;Wu, SH;Chen, YS;Lu, IL;Wu, SY;Tsai, TY;Chen, WC;Hsieh, HP;Chao, YS;Jiaang, WT
    貢獻者: Division of Biotechnology and Pharmaceutical Research
    摘要: Dipeptidyl peptidase IV (DPP-IV) inhibitors are expected to become a new type of antidiabetic drugs. Most known DPP-IV inhibitors often resemble the dipeptide cleavage products, with a proline mimic at the P I site. As off-target inhibitions of DPP8 and/or DPP9 have shown profound toxicities in the in vivo studies, it is important to develop selective DPP-IV inhibitors for clinical usage. To achieve this, a new class of 2-[3-[[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethyl]amino]-1-oxopropyl]-based DPP-IV inhibitors was synthesized. SAR studies resulted in a number of DPP-IV inhibitors, having IC50 values of < 50 nM with excellent selectivity over both DPP8 (IC50 > 100 mu M) and DPP-II (IC50 > 30 mu M). Compound 21a suppressed the blood glucose elevation after an oral glucose challenge in Wistar rats and also inhibited plasma DPP-IV activity for up to 4 h in BALB/c mice. The results show that compound 21a possesses in vitro and in vivo activities comparable to those of NVP-LAF237 (4), which is in clinical development.
    關鍵詞: Chemistry, Medicinal
    日期: 2006-01-12
    關聯: Journal of Medicinal Chemistry. 2006 Jan;49(1):373-380.
    Link to: http://dx.doi.org/10.1021/jm0507781
    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:000234575300038
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=30444442517
    顯示於類別:[蔣維棠] 期刊論文
    [伍素瑩] 期刊論文
    [李秀珠] 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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