SYNTHESIS, CHARACTERIZATION & BIOLOGICAL EVALUATION OF SOME AZETIDINE DERIVATIVES
Journal Title: International Journal of Pharmacognosy - Year 2016, Vol 3, Issue 1
Abstract
New series of N-(3-chloro-2-oxo-4-substituted-azetidine-1-yl) 2-methyl-1H-indole-3-carboxamide derivatives (VIa-d) were prepared and tested for their antibacterial and antifungal activity. The synthesis is based on the condensation of phenyl hydrazine and ethyl acetoacetate in the presence of acetic acid to ethyl (2-methyl-1H- indol-3-yl)-2-oxoacetate (III) whichonreactionwithhydrazine hydrategives 2-(2-methyl-1H- indol-3-yl)-2-oxoacetohydrazide (IV). Further condensation ofoxoacetohydrazide andsubstituted benzaldehydegavecarbohydrazide derivatives (Va-d). Finally addition of triethylamine in dry 1, 4-dioxane and chloroacetyl chloride gaveN-(3-chloro-2-oxo-4-substituted-azetidine-1-yl) 2-methyl-1H-indole-3-carboxamide derivatives (VIa-d).The structure of newly synthesized 4-Oxoazetidin Substituted derivatives have been established on the basis of spectral (IR, 1HNMR) data. These compounds were screened for antibacterial and antifungal activity against various Gram positive and Gram negative strains. All the compounds show significant antibacterial and antifungal activity.
Authors and Affiliations
Pawan Gupta
Keywords
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