肉桂酸硫酯衍生物的合成及其辐射防护作用研究  

SYNTHESIS AND RADIOPROTECTIVE ACTIVITY OF CINNAMIC ACID THIOESTER DERIVATIVE

作　　者：董欣[1] 宋金芳[1] 章琦 黄振东 励杏娣[1] 翁世芳[1] 陈永明[1] 王洪复[1] 

机构地区：[1]上海医科大学放射医学研究所

出　　处：《辐射研究与辐射工艺学报》1997年第2期105-108,共4页Journal of Radiation Research and Radiation Processing

基　　金：卫生部科学研究基金

摘　　要：为了从肉桂酸硫酯衍生物中寻找更有效的辐射损伤防护药，改变对羟基肉桂酸和芥子酸的结构，由４＇－乙氧羰基－氧基苯丙烯酸酰氯和二乙胺基代乙硫醇，在碱催化下缩合，合成了４＇－乙氧羰基－氧基－２—氯代苯丙烯酸二乙胺基代乙硫醇酯盐酸盐，以及３、４、５－三甲氧基苯丙烯酸二乙胺基代乙硫醇酯盐酸盐，经小鼠整体辐射后，早期给药试验证明：小鼠经６０Ｃｏγ射线７．５～８．０Ｇｙ照射，３０ｄ存活率治疗组比对照组提高３０％。还报道了化合物的质谱、红外及核磁共振光谱，讨论了有关化合物的ＥＳＲ光谱。In order to find more effective radioprotective agents from cinnamic acid thioester derivatives, the structure ofP - hydroxycinnamic acid and sinapic acid into4'-O- carbethoxy -2- chlorocinnamic acid diethylaminoethylthiol estenrhydrochloride and 3, 4, 5 - trimethoxyphenylpropenoic acid diethylamino ethylthiol ester hydrochloride has been changed. The main step of synthesise of these agents involved the condensation of4'- O - carbethoxy - phenylpropenoic acid chloride with diethylaminoethylthiol under base catalyst. The protective test on mice irradiated with 60 Co γ-rays of 7.5～8.0Gy was shownthat the animal survival rate was enhanced by 30% within 30 days afterirradiation in comparision with the control group. The MS, IR and NMR spectra data of cinnamic acid thioester derivative have alsobeen reported. The ESR spectra of the compound was discussed.

关 键 词：辐射防护药 肉桂酸硫酯衍生物 合成 辐射防护作用 

分 类 号：R979.6[医药卫生—药品]