2-(E)-取代苯亚甲基环戊酮缩硫代氨基脲衍生物的合成及抗癌、抗惊厥活性研究

SYNTHESIS OF 2-(E)-(UN) SUBSTITUTED BENZYLIDENE CYCLOPENTANONE THIOSEMICARBAZONE DERIVATIVES AND STUDIES ON THEIR ANTICANCER AND ANTICONVULSANT ACTIVITIES

设计、合成了14个未见文献报道的2-(E)-取代苯亚甲基环戊酮缩硫代氨基脲类新化合物并进行了抗癌、抗惊厥活性研究。初步药理试验结果表明:所有化合物体外对L1210细胞无明显杀伤潘性;化合物5i和5j对回苏灵所致小鼠惊厥有很强的抑制作用。

14 new compounds of 2-(E)-(un) substituted benzylidene cyclopentanone thiosemicarbazone derivatives were designed and synthesized as anticancer and anticonvulsant agents. Preliminary pharmacological tests showed that no compounds of this series exib.ibited cytotoxicity toward L1210 cells and that some compounds possessed certain anticonvulsant activity. In particular, 2-(E){〔3-methoxy-〔 (1-oxo-3-phenyl-2-propenyl)oxy)〕〕benzylidene}cyclopentanone thiosemicarbarzone (5i)showed significant anticonvulsant activity at a dose of 100mg/kg.