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Bioorg Med Chem Lett. 2002 Aug 19;12(16):2205-8.

N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.

Author information

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

Abstract

The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as small molecule VLA-4 antagonists is described. Potency against VLA-4 and alpha(4)beta(7) and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues.

PMID:
12127538
DOI:
10.1016/s0960-894x(02)00356-6
[Indexed for MEDLINE]

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