formylchromone and Body-Weight

A series of novel dibenzo[b,d]furan mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit Protein Tyrosine Phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Structure-activity relationship study led to the identification of potent compound 5 E which inhibited PTP1B with IC(50) value of 82+/-0.43 nM. Compound 5 E was screened in vivo as drug candidate for anti-diabetic activity using rosiglitazone maleate as the standard. Compound 5 E showed significant reduction in body weight, fed-state whole blood glucose (WBG), fasting WBG, plasma glucose and plasma cholesterol levels and non-significant reduction in fasting plasma triglyceride levels in ob/ob mice.

Topics: Animals; Blood Glucose; Body Weight; Carboxylic Acids; Catalytic Domain; Cholesterol; Drug Discovery; Furans; Hypoglycemic Agents; Inhibitory Concentration 50; Male; Mice; Protein Tyrosine Phosphatase, Non-Receptor Type 1; Substrate Specificity; Triglycerides