Facile green synthesis of 2, 4-substituted -2, 3- dihydro -1, 5 Benzothiazepine derivatives as novel anticonvulsant and central nervous system (CNS) depressant agents

Abstract

The present work reports eco friendly synthesis of 2, 4-substituted -2, 3- dihydro -1,5-benzothiazepine derivatives as novel anticonvulsant and central nervous system (CNS)depressant agents having lesser side effects. Facile, one pot efficient, solvent free microwave-assisted green synthesis of 1, 5-benzothiazepine derivatives by cyclo- condensation of 2-aminothiophenol with 1, 3-substituted-prop-2-en-1-one (2a-h) in the presence of zinc acetate as eco friendly catalyst, was investigated. The products were obtained in shorter reaction time and in better yields as compared with the conventional synthesis. The synthesized compounds (2a-h) and (3a-h) were purified by chromatographic techniques and by recrystallization from suitable solvents. Their anticonvulsant activities were evaluated by the maximal electroshock test and CNS depressant activity was evaluated by sleep deprivation test. The compounds (3a-h) have shown moderate CNS depressant activity and anticonvulsant activity. Key words: Green synthesis, 1, 5- benzothiazepines, anticonvulsant, central nervous system (CNS) depressant activity.