全哲山, 李仁利, 凌仰之. 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J. 药学学报, 1992, 27(9): 711-716.
引用本文: 全哲山, 李仁利, 凌仰之. 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J. 药学学报, 1992, 27(9): 711-716.
ZS Quan, RL Li, YZ Ling. STUDY OF THE RELATIONSHIP BETWEEN STRUCTURE AND ANTICONVULSANT ACTIVITIES OF 5-SUBSTITUTED-1-BUTRY-3-PYRAZOLIDINONES AND THEIR SYNTHESISJ. Acta Pharmaceutica Sinica, 1992, 27(9): 711-716.
Citation: ZS Quan, RL Li, YZ Ling. STUDY OF THE RELATIONSHIP BETWEEN STRUCTURE AND ANTICONVULSANT ACTIVITIES OF 5-SUBSTITUTED-1-BUTRY-3-PYRAZOLIDINONES AND THEIR SYNTHESISJ. Acta Pharmaceutica Sinica, 1992, 27(9): 711-716.

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

  • Abstract: 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.

     

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