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Published on:July 2017
Indian Journal of Pharmaceutical Education and Research, 2017; 51(4):650-655
Original Article | doi:10.5530/ijper.51.4.96

Synthesis, Characterization and Antibacterial Evaluation of Some Azole Derivatives


Authors and affiliation (s):

Manju Rani1, Shivani Sharma2, Rajani Chauhan2, Swapnil Sharma2*, and Jaya Dwivedi1

1Department of Chemistry, Banasthali University, Banasthali Rajasthan, INDIA.

2Department of Pharmacy, Banasthali University, Banasthali Rajasthan, INDIA.

Abstract:

Purpose: Tremendous rise in development of resistance to the antimicrobials has created alarming situation for researchers and clinicians. Method: In this regard, an attempt has been made to develop a series of azole derivatives using Claisen-Schmidt condensation and Micheal addition. All the newly synthesized compounds were authenticated by IR, 1H NMR, 13C NMR and MS spectral analysis. Synthesized compounds 5 (a-e) and 6 (a-e) were screened for their antibacterial activity against three Gram positive bacteria (S. aureus, B. subtilis and B. cereus), two Gram negative bacteria (E. coli and P. fluorescens) using serial dilution broth method. Results: Amongst all, Compound 5-(4-Chlorophenyl)-4-(3, 5-dimethyl-1H-pyrazol-1-yl)-3-phenylisoxazole (5 b) showed significant antibacterial activity against B. subtilis and B. cereus (IC50; 2.6 and 1.2 μg/mL) which was comparable to standard ampicillin (2.5 and 3.1 μg/mL). Conclusion: Azole derivatives were prepared using Claisen-Schmidt condensation and Micheal addition exhibits good antibacterial activity and can be further explored to confirm their suitability at clinical level.

Key words: Pyrazole, Synthesis, Claisen-Schmidt condensation, Micheal addition, Antibacterial.

 

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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