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

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.