Editorial: Phosphonate Chemistry in Drug Design and Development
Petri Turhanen, Konstantinos D. Demadis, Paweł Kafarski
Abstract
Phosphonates are surrogates of natural phosphates, but they possess direct C-P bonds and one or more phosphonic acid moieties (R-PO 3 H 2 ). These compounds are also generally used as a bioisosteres of carboxylates and serve as analogs of carboxylic acids, amino acids and peptides. Phosphon(in)ate groups are also actively mimicking the transition state during hydrolysis of amides and esters, thus being effective transition-state inhibitors. The interest in these compounds has grown immensely because of: their bioactive properties (as drugs, pro-drugs), their use as the tools for the design of enzyme inhibitors, their potential as bone-targeting drugs, their novel antibacterial and anticancer activity, their use in medical imaging and diagnostics and their phosphoantigen properties. There are several compounds containing phosphonate groups that are already in use as antiviral drugs. For example, bisphosphonates, which are active drugs against osteoporosis, demonstrate rich chemistry and biology. Applications of phosphonates cover a plethora of research fields, beyond the realm of medicinal chemistry. Examples of phosphonate compounds currently in medicinal use are given in Figure