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

作　　者：PENG Xiaoyu ZHAO Anran HUANG Kelin HU Tingju LIU Burning HUANG Yan CHEN Hailan CHAI Ling LIN Cuiwu 

机构地区：[1]School of Chemistry and Chemical Engineeting,Guangxi University,Nanning 530004,P.R.China [2]School of Animal Science and Technology,Guangxi University,Nanning 530004,P.R.China [3]Laboratory Medicine Department,First.Affiliated Hospital of Guangxi Medical University,Nanning 530021,P.R.China [4]Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards,Guangxi Institute of Traditional Medical and Pharmaceutical Sciences,Nanning 530022,P.R.China [5]China Academy of Science and Technology Development Guangxi Branch,Nanning 530022,P.R.China

出　　处：《Chemical Research in Chinese Universities》2020年第5期795-803,共9页高等学校化学研究（英文版）

基　　金：Supported by the Guangxi Natural Science Foundation,China(No.2016GXNSFBA380053);the Fund of the Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards,China(No.Guizhongzhongkai201505).

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.

关 键 词：Cafteic acid Sulphonamide LIPOPHILICITY ANTI-OXIDANT CYTOTOXICITY 

分 类 号：O62[理学—有机化学]