Background: Benzothiazine derivatives, because of their various biological activities have
attracted particular attention in Med Chem and drug discovery efforts. The synthetic modifications of
1,2-benzothiazine 1,1-dioxides have been undertaken in order to explore and identify novel compounds
or new analogues possessing promising biological activities. In our effort we have designed -oxicam
derived bezothiazine-1,2,3-triazole derivatives as potential antibacterial agents.
Methods: These compounds were synthesized via a multi-step sequence involving the Cu catalyzed azide-
alkyne cycloaddition (CuAAC) as a key step. The CuAAC proceeded at room temperature in DMF
to afford 26 novel molecules in good (70-90%) yields.
Results: All these compounds were tested for their antibacterial properties against four strains of bacterial
microorganisms and subsequently cytotoxic properties against lung and colon cancer cell lines.
The compound 4e showed activities against majority of the bacterial species used (nearly comparable
to amoxicillin, ciprofloxacin and ofloxacin against P. vulgaris) whereas 4d and 4f showed cytotoxicities
selective towards cancer cells.
Conclusion: The present bezothiazine-1,2,3-triazole framework represents a new template for the
identification of novel and potent antibacterial/anticancer agents.