Recent advances in bridged structures as 3D bioisosteres of ortho-phenyl rings in medicinal chemistry applications

Abstract

In recent years, a lot of scientists have tried to replace the phenyl ring in bioactive compounds with saturated 3D bioisosteres to obtain novel patentable structures in medicinal chemistry. Among these structures, bridged polycyclic compounds, as 3D bioisosteres of the ortho-substituted phenyl ring – a basic structural element in drugs and agrochemicals – have attracted much attention. The demand for rigid three-dimensional aliphatic skeletons to “escape from flatland” in drug discovery has prompted numerous efforts to broaden their applications and chemical spaces. This review summarises and highlights recent advances (year > 2015) in the medicinal chemistry applications of bridged polycyclic 3D bioisosteres of ortho-phenyl rings, which is expected to inspire further achievements in this area.