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Published on:June 2017
Indian Journal of Pharmaceutical Education and Research, 2017; 51(3):452-460
Original Article | doi:10.5530/ijper.51.3.73

Design and Synthesis of Novel Indolizine Analogues as COX-2 Inhibitors: Computational Perspective and in vitro Screening


Authors and affiliation (s):

Chandrashekharappa Sandeep1, Katharigatta Narayanaswamy Venugopala2,3,*, Mohammed A. Khedr3,4, Basavaraj Padmashali5,6 *, Rashmi Sanganna Kulkarni7, Rashmi Venugopala8, Bharti Odhav2

1Institute for Stem Cell Biology and Regenerative Medicine, NCBS, TIFR, GKVK, Bellary Road, Bangalore-560065, INDIA.

2Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, SOUTH AFRICA.

3Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of SAUDI ARABIA.

4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ein Helwan, Cairo 11795, EGYPT.

5Department of Chemistry, Sahyadri Science College (Autonomous), Shimoga 577 203, INDIA.

6Department of Studies and Research in Chemistry, School of Basic Sciences, Rani Channamma University, Belagavi 591 156, Karnataka, INDIA.

7Department of Chemistry, Jain University, Bangalore 560 019, INDIA.

8Department of Public Health Medicine, University of KwaZulu-Natal, Howard College Campus, Durban 4001, SOUTH AFRICA.

Abstract:

Design and synthesis of a new series of ethyl 7-methoxy-2-substituted-3-(substituted benzoyl) indolizine-1-carboxylates 2a-i was achieved and screened for their in vitro inhibitory activity against COX-2 enzyme. Compound 2a and 2c emerged as promising COX-2 enzyme inhibitor with IC50 of 6.56 and 6.94 μM respectively from the synthesized series when compared to Celecoxib and Indomethacin as selective and nonselective standards, respectively. Computational docking study identified the possible reasons for such activity that may be due to the cis configuration of the indolizines that resulted in the most stable conformation similar to that of Indomethacin.

Key words: Cox-2 Inhibition, Indolizine Analogues, Synthesis, Characterization, Molecular Docking.

 

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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.

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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