Bicyclo[1.1.1]pentane, or BCP, is a rigid cage-like framework. The two bridgehead substituents in 1,3-disubstituted BCPs extend in directions approaching 180°, making this scaffold useful in studies involving three-dimensional bioisosteric replacement of para-disubstituted benzene rings. ...
The benzene ring can restrict molecular conformation, control substituent orientation, and participate in target binding through hydrophobic interactions, π–π interactions, or cation–π interactions. It is therefore widely present in drug molecules. However, in some lead compounds, aromatic rings ...