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Azepine is a seven-membered, nitrogen-containing heterocyclic compound. It serves as an important structural scaffold and found in many natural and synthetic compounds, including several drugs, such as antipsychotic agents and antihistamines. This review article discusses the synthesis, pharmacological activities of azepine derivatives, and the structure–activity relationships (SAR) associated with them. The future prospects of azepine derivatives as therapeutic agents appear promising, as their diverse biological activities make them attractive candidates for the development of new drugs to treat various diseases.
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