Some aryl semicarbazones possessing anticonvulsant activitie

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. Correlati...

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Bibliographic Details
Published in:European journal of medicinal chemistry 1995, Vol.30 (4), p.287-301
Main Authors: Dimmock, JR, Sidhu, KK, Tumber, SD, Basran, SK, Chen, M, Quail, JW, Yang, J, Rozas, I, Weaver, DF
Format: Article
Language:English
Subjects:
anticonvulsant activity
aryl semicarbazone
molecular modeling
structure-activity relationship
X-ray crystallography
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Summary: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 σ and σ * 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.
ISSN:0223-5234
1768-3254
DOI:10.1016/0223-5234(96)88237-7