Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

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

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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Article Details

VOLUME: 9
ISSUE: 6
Year: 2012
Page: [611 - 617]
Pages: 7
DOI: 10.2174/157018012800673038
Price: $58