Convergent, parallel synthesis of a series of β-substituted 1,2,4-oxadiazole butanoic acids as potent and selective αvβ3 receptor antagonists

We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin αvβ3 and, in addition, show selectivity relative to the other β3 integrin αIIbβ3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other αv integrins such as αvβ1 and αvβ6.

Graphical abstractSynthesis of a series of potent and selective αvβ3 antagonists containing a 1,2,4-oxadiazole core is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide