1,2,3,4-Tetrahydroquinoline-containing αVβ3 integrin antagonists with enhanced oral bioavailability

Abstract Reduction of the quinoline ring in an α v β 3 antagonist yielded a 1,2,3,4-tetrahydro derivative as two diastereomers, the four isomers of which were separated by sequential chiral HPLC. Two isomers had significant α V β 3 antagonist activity with improved oral bioavailability, relative to the corresponding quinoline derivative.