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Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors |
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| Authors: | Van Goethem Sebastiaan Van der Veken Pieter Dubois Véronique Soroka Anna Lambeir Anne-Marie Chen Xin Haemers Achiel Scharpé Simon De Meester Ingrid Augustyns Koen |
| Institution: | aLaboratory of Medicinal Chemistry, University of Antwerp (UA), Universiteitsplein 1, B-2610 Antwerp, Belgium;bLaboratory of Medical Biochemistry, University of Antwerp (UA), Universiteitsplein 1, B-2610 Antwerp, Belgium;cDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Zhu Nan, Miaoli 350, Taiwan, ROC |
| 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. |
| Keywords: | DPP8 DPP9 DPP IV DPP4 DPP II DPP2 Inhibitors Allo-Ile-isoindoline Isoindoline Selectivity |
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