Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties

We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.

Graphical abstractA series of 2,5 thiazole containing compounds are described, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.Figure optionsDownload full-size imageDownload as PowerPoint slide