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ID: ALA1149358
Journal: Bioorg Med Chem Lett
Title: Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines.
Authors: Soroka A, Van der Veken P, De Meester I, Lambeir AM, Maes MB, Scharpé S, Haemers A, Augustyns K.
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.
CiteXplore: 16844373