Design, synthesis and Anti-depressant activity of some novel derivatives of Benzothiazepine

Abstract

Antidepressants are the drugs used to treat depression thereby elevates mood and modifies the behavior. The main aims in the development of new antidepressants were greater efficacy, absence of side effects, lack of toxicity in over dose and earlier onset of action. In this study, a series of novel substituted benzothiazepine was synthesized and evaluated for antidepressant-like activity by using or forced swim test (FST). This study was designed to synthesized; identify and antidepressant-like activity of novel derivatives of benzothiazepine. Our synthetic route started from substituted aromatic aldehyde which was reacted with 2-aminothiophenol and ethyl or methyl acetoacetate led to the formation of the title compounds. Total 22 benzothiazepine derivatives were synthesized. All compounds were tested for antidepressant activity by using or forced swim test (FST). All the synthesized compounds were subjected to antidepressant-like activity study on Sprague-Dawley rats by despair swim test. Imipramine was used as standard control. The results showed that all the compounds showed antidepressant activity. Among them two Compounds (A₃, A₆,B₁ B₃, and B₆) showed significant antidepressant-like activity comparing with standard control imipramine. We investigated the importance of functional group substitutions, in the structural framework of the compounds for their antidepressant-like activity. All compounds showed significant antidepressant-like activity at dose (30 mg/kg). Finally, the encouraging result of the antidepressant-like activity displayed by these compounds may be of interest for further structural modifications to the lead compound and next level studies in the hope of finding a new potent antidepressant prescription.