A Synthesis of Some New 2-Azetidinones as Potential Antitubercular Agents.

The B-Iactam drugs are still the most prescribed antibiotics used in medicine. Recently, 2-azetidinones have been assessed for anti parkinsonian I, antiinflammatory2.3, antibacterial and herbicidal activity. They also function as an enzyme inhibitors and are effective on the central nervous system. Moreover much interest has been focused on biological activities of thiazole derivatives-. Led by these considerations, synthesis of azetidinones bearing thiazole nucleus has been undertaken in order to study biodynamic behaviour of the compounds. 2Amino-4-( <x-methox yi minocarbmethox ymethy 1)thiazole 1 was prepared by using acetoacetic ester as a starting material. Compound 1 on condensation with substituted aromatic aldehydes yielded schiff bases 2a-o (Table I) which on reaction with chloroacetyl chloride and triethyl amine (as basic catalyst) afforded 2-azetidinones 3a-o (Table I) . The steps involved in the synthesis are shown in Scheme I. The titled compounds thus synthesised were screened in vitro for antitubercular activity against Mycobacterium tuberculosis H37Rv strain . The constitution of all the products was established by elemental analyses, JR, IH NMR and mass spectral data.