國家衛生研究院 NHRI:Item 3990099045/1238
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    题名: Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates
    作者: Van der Veken, P;Soroka, A;Brandt, I;Chen, YS;Maes, MB;Lambeir, AM;Chen, X;Haemers, A;Scharpe, S;Augustyns, K;De Meester, I
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: Dipeptide-derived compounds, bearing various P2 residues and a diaryl pyrrolidin-2-yl phosphonate at the PI position, were evaluated as dipeptidyl peptidase 8 (DPP8) inhibitors. With these products, irreversible inhibition of DPP8 was observed. To obtain inhibitors with an improved activity and selectivity profile, a set of selected analogues containing a diaryl isoindolin-1-ylphosphonate at P1 was synthesized and evaluated. Within this latter series, compound 2e was shown to be a potent, irreversible inhibitor of DPP8, demonstrating very low affinity for DPP IV and DPP II.
    关键词: Chemistry, Medicinal
    日期: 2007-11-15
    關聯: Journal of Medicinal Chemistry. 2007 Nov;50(23):5568-5570.
    Link to: http://dx.doi.org/10.1021/jm701005a
    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:000250809300010
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=36148930961
    显示于类别:[陳新(2002-2015)] 期刊論文

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