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N-(Arylacetyl)-biphenylalanines as Potent VLA-4 Antagonists

Li, Bing ; de Laszlo, Stephen E ; Kamenecka, Theodore M ; Kopka, Ihor E ; Durette, Philippe L ; Lanza, Jr, Thomas ; Maccoss, Malcolm ; Tong, Sharon ; Mumford, Richard A ; Mccauley, Ermengilda D ; Van Riper, Gail ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(16), pp.2141-2144 [Peer Reviewed Journal]

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Title:
N-(Arylacetyl)-biphenylalanines as Potent VLA-4 Antagonists
Author: Li, Bing ; de Laszlo, Stephen E ; Kamenecka, Theodore M ; Kopka, Ihor E ; Durette, Philippe L ; Lanza, Jr, Thomas ; Maccoss, Malcolm ; Tong, Sharon ; Mumford, Richard A ; Mccauley, Ermengilda D ; Van Riper, Gail ; Schmidt, John A ; Hagmann, William K
Description: 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.
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(16), pp.2141-2144
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/S0960-894X(02)00366-9
Subjects: Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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