2,5-Diazabicyclo[2.2.1]Heptane in Medicinal Chemistry: A Treasure Trove of Therapeutic Opportunities

The review article discusses the significance of 2,5-Diazabicyclo[2.2.1]heptane (2,5-DBH) in medicinal chemistry, highlighting its role as a valuable scaffold due to its conformational rigidity and favorable three-dimensional structure. It has been increasingly used in biologically active molecules to enhance target engagement and pharmacological profiles. The article provides a comprehensive summary of recent advancements in the synthesis and functionalization of 2,5-DBH and its derivatives, emphasizing efficient construction strategies developed over the past decade. It also explores the biological applications of 2,5-DBH-based compounds in therapeutic areas such as oncology, neurological disorders, and antimicrobial research. The review aims to guide future scaffold design and encourage further exploration of 2,5-DBH in drug discovery by integrating synthetic progress with biological insights, identifying key structure–activity relationships, and highlighting challenges and opportunities.