N-Tetrahydrofuroyl-(L)-phenylalanine Derivatives as Potent VLA-4 Antagonists.

Abstract Given the proposed involvement of VLA-4 in inflammatory processes, a program to identify orally active VLA-4 antagonists was initiated. Herein, we report the discovery of a N -tetrahydrofuroyl-( l )-phenylalanine derivative ( 17 ) and related analogues as potent VLA-4 antagonists with good oral bioavailability.