title: N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. george_doherty@merck.com
authors.forename: George A
authors.initials: GA
authors.lastname: Doherty
authors.forename: Theodore
authors.initials: T
authors.lastname: Kamenecka
authors.forename: Ermenegilda
authors.initials: E
authors.lastname: McCauley
authors.forename: Gail
authors.initials: G
authors.lastname: Van Riper
authors.forename: Richard A
authors.initials: RA
authors.lastname: Mumford
authors.forename: Sharon
authors.initials: S
authors.lastname: Tong
authors.forename: William K
authors.initials: WK
authors.lastname: Hagmann
mesh_terms: D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D010649:Phenylalanine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D039041:Integrin alpha4beta1; D016023:Integrins; D016201:Receptors, Lymphocyte Homing; D010649:Phenylalanine