ABSTRACT
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.
CHAPTER ONE
INTRODUCTION
1.1 Background of the study
The growing incidence of microbial resistance to currently used antibiotics represents a serious medical problem. Therefore, there is an urgent need to develop new classes of therapeutic agents to treat microbial infectious. Such new therapeutic agent has to exhibit a wide spectrum of biological activities. Sulphonamides, an important class of pharmaceutical compounds, exhibit a wide spectrum of biological activities1. The basic sulphonamide group [SO2, NHR]
occurs in various biologically active compounds including antimicrobial drugs,
antithyroid agents, antitumor, antibiotics and inhibitors of carbonic anhydrase2 . Sulphonamides are widely used to treat microbial infections by inhibiting the growth of Gram negative and Gram positive bacteria, some protozoa and fungi3 . Clinically, sulphonamides are used to treat several urinary tract infections and gastrointestinal infections4. Sulphonamides5 that are aromatic or heteroaromatic are responsible for the inhibition of the growth of tumor cells. They act as antitumor agents by inhibiting carbonic anhydrase activity. They are structurally similar to p– aminobenzoic acid (PABA) which is a cofactor that is needed by the bacteria for the synthesis of folic acid. Sulphonamide antibiotics inhibit the conversion of
PABA into folic acid and thus ultimately inhibit the synthesis of DNA. They are also used in veterinary medicine to treat infections in livestock6. In primary care medicine, sulphonamides are widely used in various conditions including gastrointestinal7 and urinary tract infections8. Sulphonamide is the organic framework of main focus in this research and it belongs to the family of suphur- containing compounds9, which are earlier referred to as sulpha drugs . Some of these sulpha drugs that have performed “healing magic” in the world of chemotherapy include; sulphanilamide(1), sulphadiazine(2), sulphacetamide(3), sulphamonomethoxine(4), sulphasalazine(5), sulphadoxine(6), among others. Sulphonamides have long been the subject of pharmaceutical interest as a result of their potent biological activities10
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DEPARTMENT OF PURE AND INDUSTRIAL CHEMISTRY FACULTY OF PHYSICAL SCIENCES UNIVERSITY OF NIGERIA
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