Zolpidem based compounds affects GABAA regulation in locomotor activity and sleep. Aim: The study was undertaken to evaluate the effect of Zolpidem based derivatives in mice. Synthesis, Characterizations, biological profiling and molecular docking studies were carried out to understand the biological activity and binding selectivity of the synthesized compounds. Methods: The study indicates that substituted Zolpidem based compounds were shown potent phenobarbitone induced hypnosis as well as locomotor activity throughout the study. Molecular docking study by AutoDock 4.2 MGL tools helped to understand the hypothetical selectivity of the compounds and also endowed the future prospects of de novo design for future prototype ligands. Observation: Compound 7a and 7d produced significant reduction in onset and prolongation of sleep duration induced by phenobarbitone. In the second model(Locomotor activity in actophotometer) activity was found to be maximum for 7a and 7d (30 mg/kg), produced 31.2 and 33.2 % decreased in locomotors activity, where standard drug Phenobarbitone produced 59.37% decreased in activity. Molecular docking studies also concluded the selectivity of compound 7d was appreciable in respect to the standard. The binding energy and the bond distances of phenobarbitone and Compound 7d between the target were found to be -7.24 kcal, and -6.6 kcal and 2.829 Ã?â?¦ (PRO 85), 1.896 Ã?â?¦ (PHE 78), (LEU 76) respectively. Conclusion: The study revealed the possibilities in future research of Zolpidem based derivatives for establishment of new generation CNS acting agents.
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