Fluorine in Medicinal Chemistry

Abstract

Fluorinated compounds comprise a substantial proportion in the therapeutic drugs. It is an important strategy to introduce fluorine and fluorinated substitutes in the small molecule for structure-based medicinal chemistry. They can modulate the physicochemical and pharmacokinetic properties to improve bioavailability, alter the conformation of a molecule to enhance the selectivities and binding affinity to target proteins, and block metabolically labile sites to increase the metabolic stability of drugs.

Key words: fluorine, drug design, lead optimization

Cite this article

WANG Jiang, LIU Hong. Fluorine in Medicinal Chemistry[J]. Chin. J. Org. Chem., 2011, 31(11): 1785-1798.

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