Abstract
The synthesis, SAR and biological evaluation of a series of ureas that activate glucokinase, a target for diabetes therapy as a result of its critical role in the regulation of whole-body glucose homeostasis, are described. Some of the urea-containing glucokinase activators lowered blood glucose levels in vivo following oral dosing to C57BL/6J mice.
MeSH terms
-
Administration, Oral
-
Animals
-
Blood Glucose / drug effects
-
Blood Glucose / metabolism
-
Diabetes Mellitus / drug therapy
-
Diabetes Mellitus / metabolism
-
Enzyme Activation / drug effects
-
Glucokinase / drug effects*
-
Glucokinase / metabolism*
-
Homeostasis / drug effects
-
Homeostasis / physiology
-
Humans
-
Mice
-
Molecular Structure
-
Structure-Activity Relationship
-
Urea / analogs & derivatives
-
Urea / chemical synthesis*
-
Urea / pharmacology*
Substances
-
Blood Glucose
-
Urea
-
Glucokinase