Fig 1.
Structure of biologically active imidazo[1, 2-α]pyridines.
Table 1.
Physical data of the tri-substituted-condensed-imidazopyridines and IC50 values towards the binding of PLA2.
Table 2.
Structure-activity relationships of newly synthesized tri-substituted-condensed-imidazopyridines.
Fig 2.
Synthesis of tri-substituted-condensed-imidazopyridines.
Fig 3.
IC50 values of imidazopyridine derivatives on Vipera russelli (RV) venom induced indirect haemolytic activity.
RV venom (1 μg) was pre-incubated with different concentrations of imidazopyridine derivatives for 10 min at 37°C. Assay was performed as described in methods section and IC50 values for individual imidazopyridine derivatives obtained from dose response curve is presented.
Fig 4.
Predicted interactions of imidazopyridine 3f with PLA2: PLA2 is shown as green cartoon with highlighted Trp-31 and peptide bond to Gly-32.
Co-crystallized ligand nimesulide is shown in stick representation with cyan carbon atoms. The highest scoring docking pose of compound 3f is shown in purple sticks. In silico docking predicts π-π stacking interactions with Trp-31 and additional amide-π interactions with the backbone of Gly-32.