Home | Articles
Published on:JANUARY 2018
Indian Journal of Pharmaceutical Education and Research, 2018; 52(1):110-121
Original Article | doi:10.5530/ijper.52.1.13

Synthesis, Characterization, Antidepressant Activity and Docking Studies of Some Novel Indole Bearing Azetidinone Derivatives


Authors and affiliation (s):

Deweshri Rajendrakumar Kerzare*, Sunil Sugnomal Menghani, Pramod Bhujangrao Khedekar

Department of Pharmaceutical Sciences, Computer Aided Drug Design Laboratory, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur, Maharashtra, INDIA.

Abstract:

A

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.

Key words: Indole, Azetidinone, Antidepressant activity, Docking study.

 

Articles in PDF, ePUB and Full text are attached to this page. In order to download, print or access these formats you must be logged in.
CAPTCHA
This question is for testing whether you are a human visitor and to prevent automated spam submissions.
5 + 4 =
Solve this simple math problem and enter the result. E.g. for 1+3, enter 4.




 

User login

CAPTCHA
This question is for testing whether you are a human visitor and to prevent automated spam submissions.
1 + 1 =
Solve this simple math problem and enter the result. E.g. for 1+3, enter 4.

The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

DOI HISTORY

IJPER uses reference linking service using Digital Object Identifiers (DOI) by Crossref. Articles from the year 2013 are being assigned DOIs for its permanent URLs