EVALUATION OF THE SEMICARBAZONES, THIOSEMICARBAZONES AND BIS-CARBOHYDRAZONES OF SOME ARYL ALICYCLIC KETONES FOR ANTICONVULSANT AND OTHER BIOLOGICAL PROPERTIES

A number of aryl alicyclic ketones were converted to their corresponding semicarbazones, thiosemicarbazones and bis-carbohydrazones. Anticonvulsant activity was displayed by most of the compounds in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens when given intraperitoneally to mice. However, on oral administration to rats, a marked selective activity in the MES screen only was noted. X-ray crystallography on five semicarbazones was undertaken in order to find correlations between the shapes of these molecules and anticonvulsant properties. The thiosemicarbazones displayed greater cytotoxicity to P388D1 and L1210 cells than the semicarbazones while a number of human tumors and different viruses were, in general, insensitive to representative compounds.