Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities

New arylidene-thiazolidinediones (ATZDs) were synthesized and evaluated in the alloxan-induced hyperglycemia mice model. The molecular target taken into consideration is the nuclear PPAR-γ whose crystallographic structure is available on the PDB database as 2PRG. Thus the hypoglycemic and hypolipidemic activities of compounds were compared with the result of their docking after removal of the co-crystallized ligand present in the 2PRG structure. Molecular modeling studies were carried out using the Autodock 3.0.5 and ADT 1.1 programs.

Graphical abstractNew arylidene-thiazolidinediones were synthesized and evaluated (hypoglycemic and hypolipidemic activities). The molecular targets used for docking were PPAR-α and γ, and the molecular origins of the biological activities were discussed in terms of binding energies, using rosiglitazone as the reference crystallographic ligand.Figure optionsDownload full-size imageDownload as PowerPoint slide