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Life-style changes, environmental pollution, and genetic factors have resulted in a large number of diseases to human beings. Though plant extracts have been widely used to counteract these diseases wherein the combined effect of the constituents was found to be responsible for the cure of a disease, activity of individual constituent was unknown. Further, naturally obtained heterocyclic compounds have been found to possess excellent pharmacological activity. In view of improvement of pharmacological activity, synthesis of derivatized heterocyclic compounds is considered as prime importance in drug-design. It is evident that azepine derivatives have been reported to possess a wide range of pharmacological activity. Recently, the critical reviews on pharmacology of azepines have not been reported. Here, the importance of azepine analogs and azepine-related scaffolds in drug design and discovery for various diseases such as antimicrobial, anticonvulsive, analgesic, etc. has been described. Particularly, the most remarkable azepine therapeutic molecules are emphasized via structure–activity relationship. The review specially focused on disorders of central nervous system (convulsions, pain, anxiety, Alzheimer’s, and mood disorder). In this review, it is found that heterocycle-fused azepine derivatives bestowed the most promising activity. The review might be a real help to researchers in finding efficient azepine-based pharmacological agents in future.

Update of Recently (2016–2020) Designed Azepine Analogs and Related Heterocyclic Compounds with Potent Pharmacological Activities