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.
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