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N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists
Ginger X Yang1, Linda L Chang, Quang Truong
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ginger_yang@merck.com
Bioorganic & Medicinal Chemistry Letters
|May 29, 2002
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.