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Novel 1,2,4 -Triazole Incorporated Azetidin-2-One Analogues as Anti-Tubercular Agents

Abstract

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.

Beena Thomas, Deepa George, and Jyoti Harindran

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