Abstract
Structure-activity relationship within a series of 1-aminoalkylisoquinoline-4-carboxylates as inhibitors of DPP-IV is described. A primary aminomethyl group is required to maintain biological activity. Substitution of the isoquinoline at the 6- and 8-positions with methoxy groups increases potency to 53 times that of the lead compound SDZ 029-576.
MeSH terms
-
Carboxylic Acids / chemical synthesis*
-
Carboxylic Acids / chemistry
-
Carboxylic Acids / pharmacology
-
Colonic Neoplasms
-
Dipeptidyl Peptidase 4 / metabolism*
-
Humans
-
Indicators and Reagents
-
Isoquinolines / chemical synthesis*
-
Isoquinolines / chemistry
-
Isoquinolines / pharmacology
-
Kinetics
-
Molecular Structure
-
Protease Inhibitors / chemical synthesis*
-
Protease Inhibitors / chemistry
-
Protease Inhibitors / pharmacology
-
Structure-Activity Relationship
-
Tumor Cells, Cultured
Substances
-
Carboxylic Acids
-
Indicators and Reagents
-
Isoquinolines
-
Protease Inhibitors
-
Dipeptidyl Peptidase 4