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The Role of the Phosphorus Atom in Drug Design

2018; Wiley; Volume: 14; Issue: 2 Linguagem: Inglês

10.1002/cmdc.201800693

1860-7187

Juan B. Rodríguez, Carola Gallo‐Rodriguez,

Click Chemistry and Applications

Abstract Although the phosphorus atom is found in a variety of oxidation states, most of the phosphorus‐containing molecules of pharmacological importance possess phosphorus in the form of phosphonate or phosphinate functional groups, or in a major oxidation state as a phosphate group. The most common occurrence of phosphorus in drugs is either in prodrugs or in compounds for which the phosphorus atom plays a role in the biological activity, such as in modified nucleotides, in metabolically stable analogues of metabolites bearing phosphate groups, and as bioisosteric analogues of carboxyl groups.