Abstract
A novel class of 3,6-disubstituted 2-pyridinecarboxamide derivatives was designed based on X-ray analysis of the 2-aminobenzamide lead class. Subsequent chemical modification led to the discovery of potent GK activators which eliminate potential toxicity concerns associated with an aniline group of the lead structure. Compound 7 demonstrated glucose lowering effect in a rat OGTT model.
MeSH terms
-
Amides / chemical synthesis
-
Amides / chemistry*
-
Amides / pharmacokinetics
-
Animals
-
Crystallography, X-Ray
-
Disease Models, Animal
-
Drug Discovery
-
Glucokinase / chemistry
-
Glucokinase / metabolism*
-
Hypoglycemic Agents / chemical synthesis
-
Hypoglycemic Agents / chemistry*
-
Hypoglycemic Agents / pharmacokinetics
-
Pyridines / chemical synthesis
-
Pyridines / chemistry*
-
Pyridines / pharmacokinetics
-
Rats
-
Structure-Activity Relationship
Substances
-
Amides
-
Hypoglycemic Agents
-
Pyridines
-
Glucokinase