Design Synthesis And Antidepressant Evaluation Of Some Benzofuran Substituted Chalcones

Abstract

Background: In general, the chalcones and benzofuran are exhibiting various biological activities. The evaluation of pharmacological potential of chalcones of benzofuran as antidepressant and anti-anxiety agents are explored in this research work. To get insight of the intermolecular interactions, the molecular docking studies are performed at active site of MAO-A enzyme. Aim: In this study, an attempt has been made to generate new molecular scaffold which contains chalcones of benzofuran. Methods: The derivatives was synthesized by conventional reactions and characterized by various spectrometric methods. The derivatives were evaluated for antidepressant and anti-anxiety activity by using forced swim test (FST). Molecular docking studies of the synthesized derivatives with MAO-A enzyme were performed by using Pyrx software. The pharmacokinetic study of the synthesized compounds were performed by using pk CSM software. Results (antidepressant): All the final structures were assigned on the basis of IR, 1H NMR and mass spectra. The antidepressant evaluation exhibited final derivatives 10, 16 and 22 as promising molecules with percentage decrease in immobility duration 64.21, 69.85 and 65.61 respectively. Molecular docking studies are also in agreement with pharmacological evaluation with potent compounds 16 exhibiting dock score -10.3. (Anti-anxiety): All synthesized derivatives were assigned on the basis of IR, 1H NMR and mass spectra. The anti-anxiety evaluation exhibited final derivatives 9, 15 and 21 as promising molecules with significant percentage preference to open arm are 60, 67.5 and 65.61 respectively. Molecular docking studies are also in agreement with pharmacological evaluation with potent compound 15 exhibiting dock score -9.0. Conclusion: The synthesized compound may have the potential to be developed into an antidepressant agent. The substitution of nitro and chloro groups, i.e., electron releasing groups, at R1 and R2 position, showed promising newlinexv newlineantidepressant efficacy, according to the series of compounds. Also synthesized derivatives may have the potential to be developed into an anti-anxiety agent. The substitution of nitro, i.e., electron withdrawing groups, at R1 and R2 position, showed promising anti-anxiety efficacy, according to the series of compounds. Therefore, the medicinal chemists who are involved in the creation of GABA-A inhibitors might benefit greatly from our research. newline