Abstract
Benzothiazole derivatives of thiazolidinediones (TZD) were synthesized using a modified Mitsunobu reaction of 2-(benzothiazol-2-ylmethylamino)ethanol (2) with 5-(4-hydroxybenzyl)-3-triphenylmethylthiazolidine-2,4-dione and assayed for activity on peroxisome proliferator-activated receptor (PPAR) subtypes and inhibitory activity of NO production in lipopolysaccharide-activated macrophages. Most of the tested compounds were identified as potent PPARgamma agonists, indicating their potential as drug candidates for diabetes.
Publication types
-
Comparative Study
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Benzothiazoles / chemical synthesis
-
Benzothiazoles / pharmacology
-
Cell Line
-
Dose-Response Relationship, Drug
-
Hypoglycemic Agents / chemical synthesis
-
Hypoglycemic Agents / pharmacology*
-
Lipopolysaccharides
-
Macrophages / drug effects*
-
Macrophages / metabolism
-
Mice
-
Molecular Structure
-
Nitrites / metabolism
-
PPAR gamma / agonists*
-
PPAR gamma / genetics
-
Structure-Activity Relationship
-
Thiazolidinediones / chemical synthesis
-
Thiazolidinediones / pharmacology*
-
Transfection
Substances
-
Benzothiazoles
-
Hypoglycemic Agents
-
Lipopolysaccharides
-
Nitrites
-
PPAR gamma
-
Thiazolidinediones