Abstract

1,5-benzothiazepine moiety is a very important pharmacophore bioactive compound that exhibits different biological activities. The basic constituent of benzodiazepine nucleus is diltiazem. 1,5-benzothiazepine nucleus shows different potential biological activities in various field. Our research mainly focuses on synthesis of new substituted benzodiazepine nucleus which retained anticonvulsant biological activities with less toxic effect. We synthesized successfully various substituted {1-[4-Methyl-2-substitutedphenyl-2,5-dihydro-1,5-benzothiazepin-3-yl]-ethylidene}- hydrazine (6a–6j) and chemical structures confirmed by chromatographic, electro analytical, and physiochemical methods. The preliminary screening of novel synthesized compounds anticonvulsant activity by maximal electroshock model. Based on anticonvulsant screening result, the most potent derivative was found 6c. Furthermore, preliminary safety profile of most active compound 6c was evaluated by the neurotoxicity and acute oral toxicity testing.

Key words: Acute toxicity; Anticonvulsant; Neurotoxicity; Schiff’s bases