| Title : Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads - Van der Veken_2008_Bioorg.Med.Chem.Lett_18_4154 |
| Author(s) : Van der Veken P , De Meester I , Dubois V , Soroka A , Van Goethem S , Maes MB , Brandt I , Lambeir AM , Chen X , Haemers A , Scharpe S , Augustyns K |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :4154 , 2008 |
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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. |
| PubMedSearch : Van der Veken_2008_Bioorg.Med.Chem.Lett_18_4154 |
| PubMedID: 18556199 |
| Inhibitor | Allo-Ile-isoindoline |
Van der Veken P, De Meester I, Dubois V, Soroka A, Van Goethem S, Maes MB, Brandt I, Lambeir AM, Chen X, Haemers A, Scharpe S, Augustyns K (2008)
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads
Bioorganic & Medicinal Chemistry Lett
18 :4154
Van der Veken P, De Meester I, Dubois V, Soroka A, Van Goethem S, Maes MB, Brandt I, Lambeir AM, Chen X, Haemers A, Scharpe S, Augustyns K (2008)
Bioorganic & Medicinal Chemistry Lett
18 :4154