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N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists
George A Doherty1, Theodore Kamenecka, Ermenegilda McCauley
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. george_doherty@merck.com
Bioorganic & Medicinal Chemistry Letters
|February 23, 2002
Abstract:
A series of N-arylated phenylalanine derivatives has been synthesized and has been shown to be potent inhibitors of the integrin VLA-4. N-phenyl and N-heteroaryl derivatives with hydrogen bond acceptors in the meta position demonstrated low nanomolar activity against VLA-4.