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A new series of rhodanines with phenyl substitution at the fifth position of rhodanine ring were designed targeting the PPAR-γ receptor for their possible antihyperglycemic activity. The rational design and molecular modeling studies were performed against PPAR-γ (PDB ID: 2PRG). The compounds were docked and thereafter subjected for the synthesis via dithiocarbamate formation followed by Knoevenagel condensation. Structures were confirmed by IR, NMR and Mass spectral analysis. All synthesized compounds were screened for  in vitro  glucose uptake assay using isolated hepatocytes. The Compounds  A5  and  B5  having  N -( p -methoxy benzyl) at third position of rhodanine ring showed good glucose uptake activity. These two compounds were further studied for the  in vivo  antihyperglycemic study against dexamethasone induced insulin resistance. The compounds were tested at single dose level of 10 mg/kg, per oral. The compound  B5  showed significant antihyperglycemic activity when compared with the standard drug, pioglitazone. The illustration, about the molecular design, synthesis, analysis, glucose uptake study and  in vivo  antihyperglycemic activity is reported here along with the structure activity relationships.

Rational Design, Synthesis and Evaluation of Novel Rodanine Derivatives for Antihyperglycemic Activity