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

Citation
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
Citations number
17
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
30
Issue
4
Year of publication
1995
Pages
303 - 314
Database
ISI
SICI code
0223-5234(1995)30:4<303:EOTSTA>2.0.ZU;2-M
Abstract
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.