Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents
M. V. Ramana,
Mukesh S. Sikarwar.
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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