Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ginger_yang@merck.com
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.