Quan Z S, Li R L, Ling Y Z
Department of Medicinal Chemistry, Beijing Medical University.
Yao Xue Xue Bao. 1992;27(9):711-6.
According to the quantitative structure-activity relationship studies of 3-pyrazolidinones with different substituent on positions 1 and 5 reported previously, the anticonvulsant activity is parabolically related with the total fragment constent (Fr hydrophobic parameter) of the 1 and 5 substituents 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 anticonvulsant agents. Among them 1-n-butyl-5-(p-chlorophenyl)-3-pyrazolidinone was shown to be the most potent so far synthesized.
根据先前报道的对1位和5位具有不同取代基的3-吡唑烷酮的定量构效关系研究，其抗惊厥活性与3-吡唑烷酮1位和5位取代基的总片段常数（Fr疏水参数）呈抛物线关系。最佳Fr约为5.6。因此，合成了11种新的5-取代-3-吡唑烷酮。药理试验表明它们都是有效的抗惊厥剂。其中1-正丁基-5-（对氯苯基）-3-吡唑烷酮是迄今为止合成的最有效的化合物。
