Synthesis of New Thiophene Incorporated 1, 3- Oxazepine Derivatives With Antidepressant Potential

Depression is a medical condition that can have serious consequences if it persists for an extended period. The serotonin receptor family plays a role in transporting serotonin across the synaptic cleft, with SERT (or 5-HTT) and 5-HT2A being two key members. Antagonizing these receptors would result in an antidepressant effect on individuals suffering from depression. A series of thiophene-incorporated 1,3-oxazepine derivatives were synthesized by reacting 2-amino thiophene derivatives by Gewald reaction with various substituted aromatic benzaldehydes to form Thienyl Schiff bases. The desired thiophene incorporated 1,3-oxazepine derivatives were obtained by cyclizing Thienyl Schiff bases using maleic anhydride, which was then characterized using spectroscopic techniques like IR, Mass, and 1H NMR. Among the synthesized compounds, Forced swimming and tail suspension experiments were used to assess TOM3's in vivo antidepressant efficacy. It significantly decreased immobility time in low, medium, and high doses compared to the control group. This research contributes to Sustainable Development Goal 3 (Good Health and Well-Being) by addressing mental health through the development of novel therapeutic agents. Overall, the findings of this study could assist with developing strong 5- HTT and 5-HT2AR inhibitors for the treatment of depression.