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Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists
Ihor E Kopka1, Linus S Lin, Richard A Mumford
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ihor_kopka@merck.com
Bioorganic & Medicinal Chemistry Letters
|August 6, 2002
Abstract:
A series of substituted N-(3,5-dichlorobenzenesulfonyl)-(L)-prolyl- and (L)-azetidyl-beta-biaryl beta-alanine derivatives was prepared as selective and potent VLA-4 antagonists. The 2,6-dioxygenated biaryl substitution pattern is important for optimizing potency. Oral bioavailability was variable and may be a result of binding to circulating plasma proteins.