http://jcps.bjmu.edu.cn

• Full Papers • Previous Articles     Next Articles

Study of the Relationship Between the Chemical Structure and the Anticonvulsant Activity of the 3-Pyrazolidinones

Zhe-Shan Quan, Xiao-Ping Lei, Ren-Li Li   

  1. Department of Medicinal Chemistry; Beijing Medical University, Beijing 100083
  • Received:1992-02-14 Revised:1992-07-16 Online:1992-12-15 Published:1992-12-15

Abstract: 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-substituents (∑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 synthesized. 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.

Key words: 3-Pyrazolidinones, Anticonvulsant activity, QSAR

Supporting: