Synthesis and evaluation of avermectin–imidazo[1,2-a]pyridine hybrids as potent GABAA receptor modulators

•A series of hybrid molecules based on Avermectin and imidazopyridine pharmacophores acting as GABAARs PAMs were designed.•In each of these series lead compounds were discovered using a radioligand competition binding assay.•Structural basis for activity of lead-compounds were proposed using extensive molecular docking studies.•The functional properties of highest-affinity compound as GABAARs PAM were determined by electrophysiological measurements.•Biological efficacy of hybrid molecules was demonstrated in vivo in behavioral assays using adult zebrafish.