Title of article
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: Identification of dipeptide derived leads
Author/Authors
Pieter Van der Veken، نويسنده , , Ingrid De Meester، نويسنده , , Véronique Dubois، نويسنده , , Anna Soroka، نويسنده , , Sebastiaan Van Goethem، نويسنده , , Marie-Berthe Maes، نويسنده , , Inger Brandt، نويسنده , , Anne-Marie Lambeir، نويسنده , , Xin Chen، نويسنده , , Achiel Haemers، نويسنده , , Simon Scharpe، نويسنده , , Koen Augustyns، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
4154
To page
4158
Abstract
Dipeptide derivatives bearing various P2 residues and pyrrolidine derivatives as P1 mimics were evaluated in order to identify lead structures for the development of DPP8 and DPP9 inhibitors. Structure–activity-relationship data obtained in this way led to the preparation of a series of α-aminoacyl ((2S, 4S)-4-azido-2-cyanopyrrolidines). These compounds were shown to be nanomolar DPP8/9 inhibitors with modest overall selectivity toward DPP IV and DPP II.
Keywords
DPP II , DPP2 , inhibitors , Dipeptide-derived , Selectivity , Cyanopyrrolidines , DPP8 , DPP4 , DPP9 , DPP IV , nitriles
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799738
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