1-取代苄基-5-苯基-3-吡唑烷酮衍生物的合成及抗惊厥作用

[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.

Synthesis and anticonvulsant activity of 1-substitued benzyl-5-phenyl-3-pyrazolidinones

OBJECTIVE To quantitate the structure-activity relationship(SAR) of 1-substituted benzyl-5-phenyl-3-pyrazolidone derivatives. METHODS Starting from ethyl cinnamate,ring-closing with hydrazine hydrate to gain 5-phenyl-3-pyrazolidone derivatives,then condensation and reduction to gain 1-substituted benzyl-5-phenyl-3-pyrazolidone derivatives.All the compounds were evaluated the anticonvulsant potency by maximal electroshock test. RESULTS All compounds had anticonvulsant activity in some extent,in which,non-substituted benzyl compound 1-benzyl-5-phenyl-3-pyrazolidone(2 a) was more active than other compounds. CONCLUSION Benzyl at the first position increases anticonvulsant activity of 5-phenyl-3-pyrazolidone compound.