Novel 1,2,4 -Triazole Incorporated Azetidin-2-One Analogues as Anti-Tubercular AgentsBeena Thomas1, Deepa George1*, and Jyoti Harindran2.
- *Corresponding Author:
- Deepa George
Department of Pharmaceutical Chemistry
University College of Pharmacy
Regional Institute of Medical Science and Research
Mahatma Gandhi University, Kottayam
Received date: 22/08/2014; Revised date: 16/09/2014; Accepted date: 22/09/2014
This research was focused on the rational approach in design and development of novel azetidinone derivatives comprising 1, 2, 4-triazole for anti-tubercular activity. The present work involved the preliminary in silico designing of the various novel azetidinone analogues for quantifying their drug likeness. Molecular docking experiments were carried out to identify potential drug candidates among azetidinone analogues. A new series of 1-(substituted phenyl)-4-(substituted phenyl)-3-(4H-1, 2, 4-triazol-4-yl amino) azetidin-2-ones were synthesized and evaluated for their anti tubercular activity. Different azetidinones were prepared by reacting Schiff bases with chloroacetyl chloride in the presence of catalytic amount of triethylamine. The subsequent amino azetidinones were synthesized using 4-amino 1, 2, 4-triazole. All the synthesized compounds were characterized by elemental analysis, IR, 1H NMR and mass spectral studies.3-nitro and 4-methoxy benzaldehyde analogues of azetidinone derivatives showed good anti-tubercular activity against Myco- bacterium tuberculosis H37RV strain by Alamar Blue assay method compared to standard drugs.