Author(s): S. Ramachandran, Vimeshya. N, K. Yokeshwaran, Binoy Varghese Cheriyan, M. Vijey Aanandhi


DOI: 10.5958/0974-360X.2020.00964.6   

Address: S. Ramachandran, Vimeshya. N, K. Yokeshwaran, Binoy Varghese Cheriyan, M. Vijey Aanandhi
Department of Pharmaceutical Analysis, Vels Institute of Science Technology and Advanced Studies, Pallavaram, Chennai.
*Corresponding Author

Published In:   Volume - 13,      Issue - 11,     Year - 2020

Azetidine-2-one derivatives were reported to possess antibacterial, antifungal and antidepressant activity. Pyridine derivatives were reported to possess antimicrobial activities Four-membered nitrogen heterocycles such as ß-lactam and azetidines are useful substrates in organic chemistry for the design and preparation of biologically active compounds. Azetidine-2-one derivatives were synthesized by the reaction of the Schiff base with 2-chloroacetic acid. The different substituted azetidine derivates were synthesized followed by cyclizations by C-N bond formation and by the C-C bond formation, the amine-catalyzed cycloaddition of allenoates and imines, photocycloadditions of imines and alkenes, ring contraction and expansion rearrangements, and reduction of azetidine-2-ones(ß-lactams). Synthesized compounds were evaluated for their Anti-bacterial activity against Staphylococcus aureus and Escherichia coli. The synthesized structure was established based on element analysis, IR, 1H NMR, and Mass spectral data. This indicates that new azetidine derivates can be effectively synthesized by the method mentioned in this study. Azetidine is a saturated heterocyclic organic compound containing three carbon atoms and one nitrogen atom. Indole bearing azetidine derivatives are exhibiting various biological activities. Indole bearing azetidine derivatives act as an antidepressant agent has been relatively less explored. To get intermolecular interactions, the molecular docking studies are performed at the active site of the MAO-A enzyme. This study is to generate a new molecular template by linking two pharmacophores (indole and azetidine), which are likely to exhibit antidepressant-like action in animal models. The derivatives were synthesized by spectrometric methods. Molecular docking studies of the synthesized derivatives with MAO-A enzyme were carried on by using the k-nearest neighbor genetic algorithm method. All the structures were assigned based on IR, 1H NMR, mass spectra and elemental analysis. Molecular docking studies included with pharmacological evaluation for potent compounds exhibiting dock score. These compounds may have enough potential to be developed as an antidepressant agent. It can be studied for their structural -activity relationship (SAR) studies and developed into potential molecules lead. It can make a great impact on the development of MAO-A inhibitors.

Cite this article:
S. Ramachandran, Vimeshya. N, K. Yokeshwaran, Binoy Varghese Cheriyan, M. Vijey Aanandhi. Molecular Docking Studies as Antidepressant Agents, Synthetic Techniques, Antimicrobial Screening of Azetidine-2-One Derivatives- A Review. Research J. Pharm. and Tech. 2020; 13(11):5524-5528. doi: 10.5958/0974-360X.2020.00964.6

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