Non-Peptide αvβ3 antagonists. Part 6: Design and synthesis of αvβ3 antagonists containing a pyridone or pyrazinone central scaffold

Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the β-alanine 3-substituent produced compounds that are potent and selective αvβ3 antagonists and exhibit a range of physicochemical properties.