Recent Advances in Synthesis, Mechanism of Action and Therapeutic Applications of Azepines

Review Article

Abstract

Seven-membered nitrogen heterocycles, particularly azepines, are important structural scaffolds in medicinal chemistry and drug development. The non-planar, non-aromatic nature of azepines offers unique conformational flexibility, making them valuable building blocks for pharmaceutical compounds. The expansion of five- and six-membered rings through thermal, photochemical, and microwave-assisted methods has led to diverse azepine, azepinone, and azepane derivatives. Molecular docking studies and structure-activity relationship analyses have revealed crucial insights into their binding mechanisms with therapeutic targets. Azepine-based compounds demonstrate broad pharmacological activities, including antipsychotic, antidepressant, anticonvulsant, and anticancer properties. The development of novel synthetic methodologies, particularly environmentally benign approaches, has facilitated the generation of functionalized azepine derivatives. Recent advances in transition metal catalysis and organocatalytic methods have enabled selective transformations while adhering to green chemistry principles. The incorporation of azepine moieties in drug design has resulted in over 60 approved medications, indicating their therapeutic significance. The aim of this review is to discuss about the synthesis, structure-activity relationships, and biological applications of azepine-containing compounds