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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

Author(s): M. Himaja, Asif Karigar, M. V. Ramana, D. Munirajasekhar and Mukesh S. Sikarwar

Volume 9, Issue 6, 2012

Page: [611 - 617] Pages: 7

DOI: 10.2174/157018012800673038

Price: $65

Abstract

A series of twelve novel azetedinones 4a-l have been synthesized by cyclocondensation of various Schiff bases of amino thiadiazole with chloroacetyl chloride in the presence of triethylamine. Various novel Schiff bases 3a-l were synthesized by condensation of 2-amino-5-aryl-5H-thiazolo[4,3-b]-l,3,4-thiadiazole with various aryl aldehydes. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR and mass spectra. The titled compounds 3a-l and 4a-l were evaluated for anti-tubercular activity at a concentration of 0.1-100 μg/mL by Microplate Blue Alamar Assay method. Azetedinones 4a-l showed very good inhibition against the growth of Mycobacterium tuberculosis compared to compounds 3a-l and standard Streptomycin and Pyrazinamide.

Keywords: 2-amino-5-aryl-5H-thiazolo[4, 3-b]-1, 3, 4-thiadiazoles, Antitubercular activity, Azetidin-2-ones, Schiff base


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