Synthesis, Characterization, Antidepressant Activity and Docking Studies of Some Novel Indole Bearing Azetidinone Derivatives
Deweshri Rajendrakumar Kerzare1★, Sunil Sugnomal Menghani1, Pramod Bhujangrao Khedekar1★ Corresponding author
- 1Department of Pharmaceutical Sciences, Computer Aided Drug Design Laboratory, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur, Maharashtra, INDIA.
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Deweshri Rajendrakumar Kerzare
Department of Pharmaceutical Sciences, Computer Aided Drug Design Laboratory, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur, Maharashtra, INDIA.
Received: 19-05-2017; Revised: 06-07-2017; Accepted: 05-12-2017.
Volume 52, Issue 1 · pp. 110–121 · PUBLISHED 2018 · DOI: 10.5530/ijper.52.1.13
ABSTRACT
Context: In general, indole bearing azetidinone derivatives are exhibiting various biological activities. The evaluation of pharmacological potential of the indole bearing azetidinone derivatives as antidepressant agent has been relatively less explored. 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 template by linking two pharmacophores (indole and azetidinone), which are likely to exhibit antidepressant-like action in animal models. Methods: The derivatives was synthesized by conventional reactions and characterized by various spectrometric methods. The derivatives were evaluated for antidepressant activity by using forced swim test. Molecular docking studies of the synthesized derivatives with MAO-A enzyme were carried on Vlife MDS Molecular Modelling software, version 4.3.1. by using k-nearest neighbour genetic algorithm method. Results: All the final structures were assigned on the basis of IR, 1H NMR, mass spectra and elemental analyses. The antidepressant evaluation exhibited final derivatives 26 and 36 as promising molecules with percentage decrease in immobility duration 66.82 and 65.61 respectively. Molecular docking studies are also in agreement with pharmacological evaluation with potent compounds exhibiting dock score -2.8474. Conclusion: It can be concluded that these compounds may have enough potential to be developed as antidepressant agent. It can be further studied for their structure-activity relationship (SAR) studies and developed into potential lead molecules. So our research can make a great impact on those medicinal chemists who work on the development of MAO-A inhibitors.
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Kerzare, D. R., Menghani, S. S., & Khedekar, P. B. (2018). Synthesis, Characterization, Antidepressant Activity and Docking Studies of Some Novel Indole Bearing Azetidinone Derivatives. Indian Journal of Pharmaceutical Education and Research, 52(1), 110–121. https://doi.org/10.5530/ijper.52.1.13