SYNTHESIS AND EVALUATION FOR BIOLOGICAL ACTIVITIES OF N-PYRIDIN-3-YL SUBSTITUTED [PHENYLSULPHONAMIDO] ACETAMIDE

In this study, a series of N-pyridin-3-yl substituted [phenylsulphonamido] acetamide has been synthesized. The reaction of phenylsulphonyl chloride with various amino acids in basic medium yielded phenylsulphonamido alkanoic acid which, on chlorination with thionyl chloride, gave acid chloride derivatives of phenylsulphonamido alkanoic acid in situ. The acid chloride derivatives on condensation with 3-aminopyridine gave corresponding acetamide in good to excellent yield. The compounds were characterized by FTIR, 1H-NMR and 13C-NMR and screened for antibacterial, antifugal and antioxidant activities. The result revealed that the compounds possess antibacterial activities.One the compounds, 2-[(phenylsulfonyl)amido]propanoic acid had better antibacterial activities than ciprofloxacin the reference drug while others are less active. All the compounds has less antifungal activities than ketokonazole the reference drug. 2-[(phenylsulfonyl)amido]propanoic acid had the best antioxidant properties of all the compounds.