UC84及其衍生物的合成  

Synthesis of UC 84 and Its Derivatives

作　　者：季小慎[1] 金涛[1] 苗奕[1] 刘延[1] 刘真业[1] 张华峰[1] 

机构地区：[1]空军总医院临床药理科,北京100036

出　　处：《中国药物化学杂志》2000年第3期181-183,共3页Chinese Journal of Medicinal Chemistry

摘　　要：合成了化合物 2 氯 5 (5 ,6 二氢 2 甲基 1,4 氧硫杂环己二烯 3 甲酰氨基 )苯甲酸异丙酯(UC 84) ,并以其为先导物合成了 11个未见报道的衍生物 ,活性筛选表明该类化合物有明显的抗单纯疱疹病毒 (HSV)和乙肝病毒 (HBV)Methylethyl 2 chloro 5 〔〔(5,6 dihydro 2 methyl 1,4 oxathiin 3 yl)carbonyl〕amino〕benzoate(UC 84) has the strong anti HIV activity which was found by Bader in National Cancer Institute,National Institute of Health in 1991 while screening for anti AIDS compounds.Its simple structure and obvious activity made us synthesize a series of derivatives seeking for a potential anti HBV and anti HSV compounds.According to the structure of UC 84,5,6 dihydro 2 methyl 1,4 oxathiin 3 carbonyl chloride(4) was treated with various amino compounds and 11 derivatives of UC 84 were obtained.All these compounds were evaluated,and some of them showed obvious anti HSV and anti HBV activities.The results indicated that the derivatives of 1 methylethyl 2 chloro 5 〔〔(5,6 dihydro 2 methyl 1,4 oxathiin 3 yl)carbonyl〕amino〕benzoate(UC 84) might be the potential anti HSV and anti HBV drugs in future.

关 键 词：UC84 衍生物 合成 抗病毒药 

分 类 号：R914[医药卫生—药物化学]