EVALUATION OF SOME THIOSEMICARBAZONES OF ARYL ALKYL KETONES AS CANDIDATE ANTICONVULSANT AGENTS

Thiosemicarbazones have been found to possess a wide range of biological activity including anticonvulsant activity. Structural requirements for anticonvulsant activity are thought to be electron donating groups in the presence of aryl or alkyl functional groups. Earlier work from the laboratories of Dr. J.R. Dimmock have established that some thiosemicarbazones of nuclear substituted 4-aryl-3-buten-2-ones and aryl-substituted acetophenones possess anticonvulsant 'properties and that electron donating substituents on the aryl ring were associated with bioactivity. The aim of the present investigation was the synthesis of a number of thiosemicarbazones of aryl-substituted acetophenones and some related compounds to be evaluated as potential anticonvulsant agents. In particular, the following were examined, namely, the effect on bioactivity of various electron donor substituents on the aryl ring of some aryl-substituted acetophenones, the nature of the linkage between the aryl ring and the carbon bearing the thiosemicarbazono and methyl functions, replacement of the aryl replacement of the thiosemicarbazono groups. Thiosemicarbazones can exist in the E or Z configuration and in some cases different proportions observed. Although most of the thiosemicarbazones and related derivatives examined possessed some anticonvulsant activity none possessed significant anticonvulsant activities over acetophenone thiosemicarbazone. No clear correlation between chemical structure and anticonvulsant activity could be discerned based on the anticonvulsant screening results which were available