Fluorine substituent effects (on bioactivity)

The characteristic effects of fluorine and fluoroalkyl substituents on the physico-chemical properties of molecules that are important to biological activity of fluorinated compounds are highlighted. The influence of fluorination on acidity, hydrogen-bonding, and lipophilicity that affect compound absorption and distribution is described. The current perspectives on fluorine steric interactions and the controversial role of hydrogen-bonding involving the CF bond are discussed.