血吸虫病化学预防药物4H-吡嗪并〔2,1-a〕异喹啉衍生物的合成

Studies on Chemoprophylactica of Schistosomiasis Synthesis of 4 H Pyrazino 2,1 a Isoquinoline Derivatives

合成了３３个４Ｈ－吡嗪并〔２，１－ａ〕异喹啉衍生物．动物试验结果表明，其中７个化合物对日本血吸虫病具有治疗作用，５个化合物兼有预防和治疗作用．尤以２－〔４′－（Ｎ，Ｎ－二乙基甘氨酰胺基）苯甲酰基〕－４－氧－１，２，３，６，７，１１ｂ－六氢－４Ｈ－吡嗪并〔２，１－ａ〕异喹啉为突出．它对刚钻入小鼠皮肤的血吸虫童虫及对成虫的杀灭作用与吡喹酮相仿，而且对１４ｄ的日本血吸虫童虫呈一定治疗作用．

In order to search for ideal prophylactics of schistosomiasis,thirty three title compounds were synthesized and screened against schistosomiasis japonica in mice.The results indicated that five compounds showed both prophylactic and therapeutic activity.Among them 2 4′ (N,N diethylglycylamido)benzoyl 4 oxo 1,2,3,6,7,11b hexahydro 4 H pyrazino 2,1 a isoquinoline was the most active.It is as effective as praziquantel against 2 h old schistosomula and adult worms,and also showed certain activity against 14 d old schistosomula.