EVALUATION OF THE SEMICARBAZONES, THIOSEMICARBAZONES AND BIS-CARBOHYDRAZONES OF SOME ARYL ALICYCLIC KETONES FOR ANTICONVULSANT AND OTHER BIOLOGICAL PROPERTIES
Jr. Dimmock et al., EVALUATION OF THE SEMICARBAZONES, THIOSEMICARBAZONES AND BIS-CARBOHYDRAZONES OF SOME ARYL ALICYCLIC KETONES FOR ANTICONVULSANT AND OTHER BIOLOGICAL PROPERTIES, European journal of medicinal chemistry, 30(4), 1995, pp. 303-314
A number of aryl alicyclic ketones were converted to their correspondi
ng semicarbazones, thiosemicarbazones and bis-carbohydrazones. Anticon
vulsant activity was displayed by most of the compounds in the maximal
electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screen
s when given intraperitoneally to mice. However, on oral administratio
n to rats, a marked selective activity in the MES screen only was note
d. X-ray crystallography on five semicarbazones was undertaken in orde
r to find correlations between the shapes of these molecules and antic
onvulsant properties. The thiosemicarbazones displayed greater cytotox
icity to P388D1 and L1210 cells than the semicarbazones while a number
of human tumors and different viruses were, in general, insensitive t
o representative compounds.