Synthesis of Some Novel 1, 5-Benzothiazepine Derivatives Biological Screening For Anticonvulsant Activity

ABSTRACTThe presence of recurrent seizures is responsible for epilepsy, further which has been characterized in the era. A seizure can be mention as “an episodic disturbance of movement, feeling, or consciousness caused by sudden synchronous, inappropriate, and excessive electrical discharges in the cerebral cortex” 1. Epileptic convulsions are expected to have negative consequences on the patient’s psychological and social life such as relationships, education and employment. Uncontrolled seizures are associated with physical and psychosocial morbidity, dependent behavior, poor quality of life and an increased risk of sudden unexpected death. The heterocyclic compound is a potential compound for the development of chemotherapeutic and pharmacotherapeutic agents containing nitrogen and sulphur atoms2. Therefore the present investigation was made in direction to the synthesis of some newer 1, 5-benzothiazepine derivatives and their evaluation for anticonvulsant activity. Physicochemical and elemental analysis of all the 1, 5-benzothiazepine (1B-10B) is confirmed with a preliminary study like melting point, elemental analysis and hyphenated tool namely IR, NMR and Mass spectroscopy. Firstly Primarily, ?,?-unsaturated carbonyl compounds or chalcones were prepared by the well-known Claisen-Schmidt condensation of acetophenones and substituted aldehyde by using alcoholic KOH (10%) at room temperature. By adding diazonium salt in substituted chalcone ,substituted diazonium chalcone was prepared. A yield mixture and 0.01 mole of substituted mercapto anilines was dissolved in 2-methoxyethanol to get final product 1, 5-benzothiazepine derivatives. These molecules were evaluated for possible anticonvulsant activity. Anti-seizure activities of all synthesized compounds 101B to 110B were explored using MES. The synthesized compounds from (101B to 110B) 108B and 109B had shown significant activity against the tonic seizure as compared to the other synthesized compounds. Keywords