镇静抗癫痫新药SC_(1001)衍生物的合成及其抗惊厥活性

SYNTHESIS OF NEW SEDATIVE AND ANTIEPILETIC SC1001 DERIVATIVES AND ITS ANTICONVULSANT ACTIVITY

作者依据2-氯-4-溴-α-甲基肉桂酸(SC1001)的明显镇静、安眠及抗癜痫作用,设计合成了SC1001甲酯及14个酰胺衍生物,均为未知化合物,目的在于寻求活性更佳的化合物。所有化合物经抗惊厥药物筛选方法筛选,结果SC1001酰丙胺(6)、SC1001酰异丙胺(7)和SC1001酰丁胺(8)的抗惊厥活性均优于SC1001,其中化合物(8)最好。

Fifteen derivatives of2-chloro-4-bromo-α-methylcinnamic acid(SC1001) were synthesized. Theirc hemicalstructures were identified with IR, andPMR. All the fifteen synthesized titlecompounds were evaluated as anticonv-ulsants inmice via the AntiepilepticDrug Development Program. Anticonvul-sant activity of the amides of SC1001respectively with N-propyl, N-isopropyl.and N-butyl (8) was better than that ofSC1001, and (8) was the best.