| Title : Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors - Kaczanowska_2010_ACS.Med.Chem.Lett_1_530 |
| Author(s) : Kaczanowska K , Wiesmuller KH , Schaffner AP |
| Ref : ACS Med Chem Lett , 1 :530 , 2010 |
|
Abstract :
A collection of novel aminomethyl-pyridines was designed, synthesized, and investigated as potential inhibitors of DPP-4. Optimization of the screening hit afforded a number of 5-aminomethyl-pyridines with inhibitory activity in the nanomolar range. Selected DPP-4 inhibitors were further evaluated for their selectivity over the closely related peptidase DPP-8. 5-Aminomethyl-4-(2,4-dichloro-phenyl)-6-methyl-pyridine-2-carboxylic acid cyanomethyl-amide showed high potency and excellent DPP-4 selectivity [IC50: 10 (DPP-4) and 6600 nM (DPP-8)] and no toxicity in mammalian cell culture. |
| PubMedSearch : Kaczanowska_2010_ACS.Med.Chem.Lett_1_530 |
| PubMedID: 24900243 |
| Inhibitor | CHEMBL1688431-Cpd4e7 |
Kaczanowska K, Wiesmuller KH, Schaffner AP (2010)
Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors
ACS Med Chem Lett
1 :530
Kaczanowska K, Wiesmuller KH, Schaffner AP (2010)
ACS Med Chem Lett
1 :530