Synthesis, preliminary anticonvulsant and toxicity screening of substituted 3-(Dimethyl/Diethylamino)-{1-[4-methyl-2-substitutedphenyl-2,5-dihydro-1,5-benzothiazepin-3-yl]}propan-1-one

Background; 1,5-benzothiazepine moiety is a very important pharmacophore bioactive compound that exhibits different biological activities. By the literature review basic structure requirements for anticonvulsant activity contains molecular weight less than 500, Oil/water distribution coefficient 5, Hydrogen bond donors more 5 and acceptor 10. Aim of study: study to synthesize novel series nucleus containing Mannich bases which retained activities with toxic effect. Materials & methods: We synthesized successfully various substituted 3-(Dimethyl/Diethylamino)-{1-[4-Methyl-2 substitutedphenyl-2,5-dihydro-1,5 benzothiazepin-3-yl]}propan-1-one (6a-6t). Completion chemical reaction was monitored by thin layer chromatography on silica gel G coated plates final compounds were purified recrystallisation methanol. The confirmed chromatographi, electro analytical physiochemical analysis. Results discussion: All screened maximum electroshock induced seizure against Phenytoin as standard. showed significant activity. most potent found 3-(Dimethylamino)-{1-[3-chlorophenyl-4-methyl-2, 5-dihydro-1,5-benzothiazepin-3-yl]}propan-1-one (6e). Further, preliminary safety profile 6e evaluated acute oral toxicity neurotoxicity testing.