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Bioorg Med Chem Lett. 2002 Aug 19;12(16):2141-4.

N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.

Author information

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

Abstract

A series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4 antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further optimization led to several highly potent compounds (IC(50) <1 nM). Evaluation of rat pharmacokinetic revealed generally high clearance.

PMID:
12127523
[Indexed for MEDLINE]

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