| Title : Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines - Soroka_2006_Bioorg.Med.Chem.Lett_16_4777 |
| Author(s) : Soroka A , Van der Veken P , De Meester I , Lambeir AM , Maes MB , Scharpe S , Haemers A , Augustyns K |
| Ref : Bioorganic & Medicinal Chemistry Lett , 16 :4777 , 2006 |
|
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. |
| PubMedSearch : Soroka_2006_Bioorg.Med.Chem.Lett_16_4777 |
| PubMedID: 16844373 |
Soroka A, Van der Veken P, De Meester I, Lambeir AM, Maes MB, Scharpe S, Haemers A, Augustyns K (2006)
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines
Bioorganic & Medicinal Chemistry Lett
16 :4777
Soroka A, Van der Veken P, De Meester I, Lambeir AM, Maes MB, Scharpe S, Haemers A, Augustyns K (2006)
Bioorganic & Medicinal Chemistry Lett
16 :4777