| Literature DB >> 18556199 |
Pieter Van der Veken1, 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.
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 alpha-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.Entities:
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Year: 2008 PMID： 18556199 DOI： 10.1016/j.bmcl.2008.05.080
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823