Synthesis and Evaluation of Novel Peroxisome Proliferator Activated Receptor-γ (PPAR-γ) Agonists for the Treatment of Diabetes

Abstract

A series of novel thiazolidinedione derivatives as peroxisome proliferator activated receptor-gamma (PPAR-gamma) agonists bearing different fatty acid esters and amides as substituents in the positions 3 and 4 of the benzylidene moiety have been designed, synthesized and tested as potential antihyperglycemic agents. The compounds containing stearic acid (A1TU, A2TU, A3TU, A2TS and A3TS) exhibited the maximum activity (64.7-70.3 % BG reduction) among all the synthesized compounds. The capric acid containing compounds (D2TU and D3TU) showed the minimum activity (28.8-36.3 % BG reduction) with exception of D1TU and D1TS which exhibited 57.2 % and 48.7 % of BG reduction respectively. Compounds containing myristic acid (B1TU, B2TU, B3TU, B1TS and B3TS) and palmitic acid (C1TU, C2TU, C3TU, C2TS and C3TS) were found to be less active than stearic acid derivatives but more active than capric acid derivatives.

Keywords: PPAR-γ, thiazolidinedione, fatty acids, antihyperglycemic activity

Cite this Article

Ashwani Kumar, Sahil Kumar. Synthesis and Evaluation of Novel Peroxisome Proliferator Activated Receptor-γ (PPAR-γ) Agonists for the Treatment of Diabetes. Research & Reviews: Journal of Toxicology. 2016; 6(2): 1–12p.