Abstract
A series of substituted N-(3,5-dichlorobenzenesulfonyl)-( l)-prolyl- and ( l)-azetidyl-β-biaryl β-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.
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