Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

Title:Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

Volume: 9 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Himaja M., Karigar Asif, V. Ramana M., Munirajasekhar D. and S. Sikarwar Mukesh, Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents, Letters in Drug Design & Discovery 2012; 9 (6) . https://dx.doi.org/10.2174/157018012800673038