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Bioorg Med Chem Lett. 2002 Sep 2;12(17):2415-8.

Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ihor_kopka@merck.com

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.

PMID:
12161146
DOI:
10.1016/s0960-894x(02)00460-2
[Indexed for MEDLINE]

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