Synthesis of Caffeic Acid Sulphonamide Derivatives and Preliminary Exploration of Their Biological Applications

摘要

Stnictural modification of native compounds is an effective way to develop new dmgs with increased pharmacological activities and improved material characteristics.In this study,cafteic acid sulphonamide derivatives(CSs)were synthesised by conjugating sulphonamides to the backbone of cafteic acid.The structures of these derivatives were elucidated by means of Fourier traiisfonn infrared spectroscopy(FTIR),1H NMR,13C NMR,and electrospray ionization mass spectroscopy(ESI-MS).A content determination method was established by ultraviolet detection.The lipophilicity,2,2-diphenyl-l-picrylhydrazy free radical(DPPH)scavenging capacity,anti-coagulant eitects,anti-bacterial activity,cytotoxicity,in vitro anti-proliterative activity against tumour cells,and the ability of the compounds to promote the proliferation of chondrocytes were evaluated.The results indicate that CSs exliibit strong DPPH scavenging activity,high lipophilicity,good anti-coagulant activities,wide anti-bacterial activity range,low cytotoxicity,and an excellent ability to promote chondrocyte proliferation.