[摘要] [目的] 阐明1-取代苄基-5-苯基-3-吡唑烷酮衍生物的构效关系. [方法] 以肉桂酸乙酯为原料， 与水合肼环合反应得5-苯基-3-吡唑烷酮，再经缩合及还原得6种1-取代苄基-5-苯基-3-吡唑烷酮衍生物，采用最大电惊厥法测定其抗惊厥活性. [结果] 所合成的化合物均有抗惊厥活性，其中苄基环上无取 代的1-苄基-5-苯基-3-吡唑烷酮的抗惊厥作用最强. [结论] 5-苯基-3-吡唑烷酮1位引入苄基可增强其 抗惊厥作用.

    [关键词] 吡唑类;抗惊厥药;合成

    Synthesis and anticonvulsant activity of1-substitued benzyl-5-phenyl-3- pyrazolidinones

    ZHANG Lei，YIN Xiu-mei *

    (Department of Pharmaceutical Chemistry，Yanbian University College of Pharmacy，Yanji133000，Jilin，China)

    ABSTRACT:OBJECTIVE To quantitate the structure-activity relationship(SAR)of1-substituted benzyl-5-phenyl-3-pyrazolidone derivatives.METHODS Starting from ethyl cinnamate ......