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我们曾用Topliss方法及Fibonacci寻找法设计并合成了14个5-苯基1-取代吡唑烷酮化合物。其中有11个化合物具有抗惊活性,即1位取代基分别是:H,-nC_5H_(11),—(?),n—C_3H_7,—iC_3H_7—CH_2—ph,—CH_2Ph—4Cl,—CH_2—Ph—3Cl,—CH_2—Ph3,4Cl_2,—CH_2—Ph—4CF_3,—CH_2—ph3、4—O—CH_2—O-。(11个化合物的生物活性及参数值均报道于文献1)。对这11个化合物进行结构与抗惊活性关系的研究,发现由于5—苯基的引入,增加了吡唑烷酮的亲脂性,
We have designed and synthesized 14 5-phenyl 1-substituted pyrazolidinone compounds using the Topliss method and the Fibonacci search method. Among them, 11 compounds have anti-shock activity, that is, 1-substituent is H, -nC_5H_ (11), - (?), N_C_3H_7, -iC_3H_7-CH_2-ph, -CH_2Ph-4Cl, Ph-3Cl, -CH_2-Ph3,4Cl_2, -CH_2-Ph-4CF_3, -CH_2-ph3,4-O-CH_2-O-. (The biological activities and parameter values of 11 compounds are reported in literature 1). The 11 compounds were studied on the relationship between structure and anti-shock activity and found that due to the introduction of 5-phenyl, the lipophilicity of pyrazolidone increased,