Selected Applications of Spirocycles in Medicinal Chemistry

This chapter highlights a number of useful applications of spirocycles in medicinal chemistry and their impacts in drug discovery. It presents several important literature examples that illustrate some key applications of spirocycles for the development of bioactive molecules of relevance to the pharmaceutical sector. Spirocycles have also been used to modulate physicochemical properties and pharmacokinetics of biomolecules, including aqueous solubility and metabolic stability. A broad class of spirocycles which has attracted significant interest in drug discovery are those containing a four-membered ring. The unique range of properties provided by spirocycles has resulted in the development of a large number of bioactive lead compounds. The introduction of spirocycles has proven valuable for optimizing key parameters such as conformational freedom/restriction, lipophilicity, solubility, basicity, and metabolic stability, in addition to opportunities in exploring novel chemical and IP space.