Phosphine oxides belong to a chemical class seldom employed in drug design. However, the FDA-approval of Brigatinib drug (ARIAD Pharm.) in 2017 may further inspire the application of this unique functional group in medicinal chemistry. The highly ionic P=O bond imparts a number of important drug-like properties, including decreased lipophilicity, increased aqueous solubility, H-bond acceptor ability, and high metabolic stability. Herein we have designed and synthesized a library of phosphine oxide derivatives for drug design.
- chemically stable
- metabolically stable
- H-bond acceptor
- increases solubility
- decreases lipophilicity
- >30 unique P(O)Me2-containing derivatives on a 5-50 g scale from our stock.
Design and a full list of compounds you can find at our web-page in MedChem highlights section or by downloading the attached white paper.