Title : Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors - Van Goethem_2008_Bioorg.Med.Chem.Lett_18_4159 |
Author(s) : Van Goethem S , Van der Veken P , Dubois V , Soroka A , Lambeir AM , Chen X , Haemers A , Scharpe S , De Meester I , Augustyns K |
Ref : Bioorganic & Medicinal Chemistry Lett , 18 :4159 , 2008 |
Abstract :
To obtain selective and potent inhibitors of dipeptidyl peptidases 8 and 9, we synthesized a series of substituted isoindolines as modified analogs of allo-Ile-isoindoline, the reference DPP8/9 inhibitor. The influence of phenyl substituents and different P2 residues on the inhibitors' affinity toward other DPPs and more specifically, their potential to discriminate between DPP8 and DPP9 will be discussed. Within this series compound 8j was shown to be a potent and selective inhibitor of DPP8/9 with low activity toward DPP II. |
PubMedSearch : Van Goethem_2008_Bioorg.Med.Chem.Lett_18_4159 |
PubMedID: 18556198 |
Inhibitor | Allo-Ile-isoindoline |
Van Goethem S, Van der Veken P, Dubois V, Soroka A, Lambeir AM, Chen X, Haemers A, Scharpe S, De Meester I, Augustyns K (2008)
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors
Bioorganic & Medicinal Chemistry Lett
18 :4159
Van Goethem S, Van der Veken P, Dubois V, Soroka A, Lambeir AM, Chen X, Haemers A, Scharpe S, De Meester I, Augustyns K (2008)
Bioorganic & Medicinal Chemistry Lett
18 :4159