Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines |
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| Authors: | Soroka Anna Van der Veken Pieter De Meester Ingrid Lambeir Anne-Marie Maes Marie-Berthe Scharpé Simon Haemers Achiel Augustyns Koen |
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| Institution: | Laboratory of Medicinal Chemistry University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium. |
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| Abstract: | In this paper, we report the synthesis of diastereomerically pure N-(4-substituted-2,4-diaminobutanoyl)piperidines. These compounds were prepared to investigate the influence of the 4-substitution on the dipeptidyl peptidase II (DPP II) activity and selectivity of the parent N-(2,4-diaminobutanoyl)piperidine. The (4S)-methyl compound showed subnanomolar inhibition, comparable with the parent compound. The (4R)-methyl group or bigger substituents decreased the activity. |
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