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.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1995年第2期55-59,共5页
Chinese Journal of Pharmaceuticals
关键词
抗棘球蚴药物
阿苯达唑亚砜
阿苯达唑砜
合成
antihydatidosis drugs,methyl 5(6)-substituted phenyl(alkyl) thio(sulfinyl,sulfonyl) benzimidazole-2-carbamates
