Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

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.