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N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists
Bing Li1, Stephen E de Laszlo, Theodore M Kamenecka
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. bing_li@merck.com
Bioorganic & Medicinal Chemistry Letters
|July 20, 2002
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.