Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365029 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Pieter Van der Veken, Ingrid De Meester, Véronique Dubois, Anna Soroka, Sebastiaan Van Goethem, Marie-Berthe Maes, Inger Brandt, Anne-Marie Lambeir, Xin Chen, Achiel Haemers, Simon Scharpé, Koen Augustyns,