SOME ARYL SEMICARBAZONES POSSESSING ANTICONVULSANT ACTIVITIES

被引:93
作者
DIMMOCK, JR
SIDHU, KK
TUMBER, SD
BASRAN, SK
CHEN, M
QUAIL, JW
YANG, J
ROZAS, I
WEAVER, DF
机构
[1] UNIV SASKATCHEWAN, COLL PHARM & NUTR, SASKATOON, SK, CANADA
[2] UNIV SASKATCHEWAN, DEPT CHEM, SASKATOON, SK S7N 0W0, CANADA
[3] QUEENS UNIV, DEPT CHEM, KINGSTON, ON K7L 3N6, CANADA
基金
英国医学研究理事会;
关键词
ARYL SEMICARBAZONE; ANTICONVULSANT ACTIVITY; X-RAY CRYSTALLOGRAPHY; MOLECULAR MODELING; STRUCTURE ACTIVITY RELATIONSHIP;
D O I
10.1016/0223-5234(96)88237-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A number of aryl semicarbazones displayed anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens when administered intraperitoneally to mice. When given by the oral route to rats, protection was afforded in the MES but not scPTZ tests. Correlations were noted between the sigma and sigma* values of the aryl substituents, the interplanar angles made by the aryl rings with the adjacent carbimino groups and the shapes of certain semicarbazones determined by X-ray crystallography, and the activities in the rat oral MES screen. Molecular modeling studies revealed a number of statistically significant descriptors which contributed to anticonvulsant activity.
引用
收藏
页码:287 / 301
页数:15
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