抗棘球蚴药物研究：阿苯达唑代谢物及其类似物的合成  

STUDY ON DRUGS AGAINST HYDATIDOSIS:SYNTHESIS OF METABOLITES AND ANALOGUES OF ALBENDAZOLE

作　　者：黄立信[1] 胡金玉[1] 

机构地区：[1]中国预防医学科学院寄生虫病研究所

出　　处：《中国医药工业杂志》1995年第2期55-59,共5页Chinese Journal of Pharmaceuticals

摘　　要：合成了共２５个阿苯达唑代谢物及其类似物．感染棘球蚴小鼠试验表明，其中７个化合物对细粒棘球蚴有较好的作用，而以阿苯达唑亚砜（１３）效果最好，治疗剂量仅为阿苯达唑的一半，抗小鼠继发性细粒棘球蚴病的疗效高于后者．另一个代谢物阿苯达唑砜则无杀虫作用。Twenty-five metabolites and analogues of albendazole were synthesized for screening drugs against Echinococcus granulosus cysts in mice and their biological activities were compared.The results of preliminary screening tests showed that compounds 4,5,7,8,11,13,and 20 exhibited better effects against hydatidosis in mice.Among them,albendazole sulfoxide(13)was more effective than the others including albendazole even administered at a half dose of the latter.Nevertheless,an other major metabolite,albendazole sulfone,possessed no effect.

关 键 词：抗棘球蚴药物 阿苯达唑亚砜 阿苯达唑砜 合成 

分 类 号：TQ463.4[化学工程—制药化工]