Metabolically Stabilized Lipophilic Groups

Protein binders frequently contain lipophilic groups that interact with hydrophobic surfaces within the protein interior. However, incorporating such groups into drug candidates often results in reduced metabolic stability, posing significant challenges for advancing effective bioactive molecules to clinics. Spirocyclic groups provide a viable solution to this issue. They increase volume and lipophilicity while being much less prone to metabolic clearance. Enamine’s collection of spirocyclic groups features a diverse range of ring sizes and molecular topologies as exemplified by the collection of spiroalkyl amines.