The Hansch approach was used in the quantitative structure anticonvulsant activity studies of the previously synthesized 1-substituted-and 1.5-disubstituted-3-pyrazo- lidinones.Correlation analysis predicted that 1.5-...The Hansch approach was used in the quantitative structure anticonvulsant activity studies of the previously synthesized 1-substituted-and 1.5-disubstituted-3-pyrazo- lidinones.Correlation analysis predicted that 1.5-disubstituted-3-pyrazoljdinones in which 1- substituent is n-propyl but not benzyl.with the total hydrophobic constant of 1-and 5-sub- stituents(∑л)equals to 4.5(optimum value)will have the most potent activity.On the basis of this analysis eleven 5-substituted and I-n-butyl-5-substituted-3-pyrazolidinones were syn- thesized.Pharmacological tests indicated that the prediction of the Hansch analysis of the 3- pyrazolidinones is correct.The Hansch analysis,by including these 11 compounds,gives an almost identical correlation with that previously obtained.展开更多
文摘The Hansch approach was used in the quantitative structure anticonvulsant activity studies of the previously synthesized 1-substituted-and 1.5-disubstituted-3-pyrazo- lidinones.Correlation analysis predicted that 1.5-disubstituted-3-pyrazoljdinones in which 1- substituent is n-propyl but not benzyl.with the total hydrophobic constant of 1-and 5-sub- stituents(∑л)equals to 4.5(optimum value)will have the most potent activity.On the basis of this analysis eleven 5-substituted and I-n-butyl-5-substituted-3-pyrazolidinones were syn- thesized.Pharmacological tests indicated that the prediction of the Hansch analysis of the 3- pyrazolidinones is correct.The Hansch analysis,by including these 11 compounds,gives an almost identical correlation with that previously obtained.
