Background:
Thiazolidinediones and its bioisostere, namely, rhodanines have become
ubiquitous class of heterocyclic compounds in drug design and discovery. In the present study, as
part of molecular design, a series of novel glitazones that are feasible to synthesize in our laboratory
were subjected to docking studies against PPAR-γ receptor for their selection.
Methods and Results:
As part of the synthesis of selected twelve glitazones, the core moiety, pyridine
incorporated rhodanine was synthesized via dithiocarbamate. Later, a series of glitazones were
prepared via Knovenageal condensation. In silico docking studies were performed against PPARγ
protein (2PRG). The titled compounds were investigated for their cytotoxic activity against 3T3-L1
cells to identify the cytotoxicity window of the glitazones. Further, within the cytotoxicity window,
glitazones were screened for glucose uptake activity against L6 cells to assess their possible antidiabetic
activity.
Conclusion:
Based on the glucose uptake results, structure activity relationships are drawn for the
title compounds.
Novel glitazones as PPARγ agonists: molecular design, synthesis, glucose uptake activity and 3D QSAR studies
