Pyridone derivatives as potent and selective VLA-4 integrin antagonists

A novel series of pyridone inhibitors has been identified through pharmacophore analysis, as potent antagonists of VLA-4.

Graphical abstractEmploying molecular overlay studies of our initial leads with known VLA-4 antagonists has led to the hypothesis of a novel pharmacophore. Subsequent design and synthesis of analogues exploiting this hypothesis has afforded a novel series of potent and selective VLA-4 antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide