苯并硫氮杂卓类化合物作为抗血吸虫药物的研究  

Anti-schistosomal activity of benzothiazepine derivatives

作　　者：刘奉友 陈晶磊[1] 乔春华[1] 

机构地区：[1]苏州大学医学部药学院,江苏苏州215123

出　　处：《化学研究与应用》2016年第4期442-448,共7页Chemical Research and Application

摘　　要：体外筛选实验发现:苯并硫氮杂卓类化合物B_(30),在50μM浓度时,可以完全杀灭日本血吸虫。本文以B_(30)为先导化合物,通过药物化学中的生物电子等排原理对其进行结构改造,设计并合成了11个B_(30)的类似物。对这些化合物进行体外抗血吸虫效果的评价,发现其中一个化合物A9的活性较好:其对血吸虫童虫和成虫的IC50分别为7.30μM和12.0μM,较先导化合物B_(30)IC50值降低了一倍。Discovered from in vitro screening,a benzothiazepine type compound B_（30）,at 50 μM killed all tested Schistosoma japonicum.In this research,B_（30） was used as a lead compound,11 analogues were designed and synthesized.Their in vitro anti-schistosomal activities were evaluated.Among these compounds,A9 was found to exhibit higher worm killing activity,with IC50 values of 7. 30 μM and 12. 0 μM against 14-day-old and 35-day-old schistosomes,respectively,which were half value of compound B_（30）,suggesting compound A9 was more effective.

关 键 词：苯并硫氮杂卓类化合物 日本血吸虫 抗血吸虫药物 

分 类 号：O626.29[理学—有机化学]