Synthesis and Evaluation of the Hypoglycemic and Hypolipidemic Activity of Novel Arylidene Thiazolidinedione Analogson a Type 2 Diabetes Model

Abstract

Thiazolidinediones (TZDs) represent a new class of antidiabetic drugs having an insulin sensitizing effect in patients with type2 diabetes. This article reports synthesis and evaluation of two novel derivatives of rosiglitazone (an effective drug of 5-arylidene-2,4-thiazolidinedione family) containing chlorophenyl instead of phenyl, s-triazine-morpholine instead of pyridine, and a double bond adjacent to the TZD ring (compounds V and VI).The new chemical entities were tested for antihyperglycemic and antihyperlipidemic activity on the alloxan-induced diabetic rat model. Results indicated that both new drugs showed hypoglycemic and hypolipidemic activity comparable to the control group, but compound V exhibited more significant blood lipid lowering activity as compared to other groups. Moreover, the new drugs displayed high efficiency in increasing HDL level and also HDL/LDL ratio, as good lipid profiles compared to others, which provide useful results for the interpretation of hypolipidemic activity of 2,4-thiazolidinedionedrugs.