5-取代-1-正丁基-3-吡唑烷酮类化合物的合成及抗惊作用的构效关系  

STUDY OF THE RELATIONSHIP BETWEEN STRUCTURE AND ANTICONVULSANT ACTIVITIES OF 5-SUBSTITUTED-1-BUTRY-3-PYRAZOLIDINONES AND THEIR SYNTHESIS

作　　者：全哲山[1] 李仁利[1] 凌仰之[1] 

机构地区：[1]北京医科大学药化教研室

出　　处：《药学学报》1992年第9期711-716,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金;国家医药总局资助课题

摘　　要：1-正癸基-3-吡唑烷酮是一种新的抗惊活性物质。杜明慧、雷小平等相继合成了一系列3-吡唑烷酮类化合物,结果,1-正丙基-5-对氟苯基-3-吡唑烷酮的抗惊作用最强(EP_(50)=14.7 mg/kg)。为了继续研究1位和5位取代基对抗惊活性的影响,我们将前人合成的35个化合物(表1中化合物1～35)进行了Hansch分析得到以下方程:According to the quantitative structure-activity relationship studies of 3-pyrazolidi-nones with different substituent on positions 1 and 5 reported previously, the anticonvulsant activity isparabolically related with the total fragment constent ( Fr hydrophobic parameter) of the 1 and 5 sub-stituents of 3-pyrazolidion. The optimum Fr was about 5. 6. Therefore, eleven new 5-substituted-3-pyrazolidinones have been synthesized. Pharmacological test showed that they are all potent anticonvul-sant agents. Among them 1-n-butyl-5-(p-chlorophenyl)-3-pyrazolidinone was shown to be the mostpotent so far synthesized.

关 键 词：吡唑烷酮 抗惊作用 

分 类 号：R971.3[医药卫生—药品]