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N-Aryl-prolyl-dipeptides as potent antagonists of VLA-4

Kamenecka, Theodore M ; Lanza, Jr, Thomas ; de Laszlo, Stephen E ; Li, Bing ; Mccauley, Ermengilda D ; Van Riper, Gail ; Egger, Linda A ; Kidambi, Usha ; Mumford, Richard A ; Tong, Sharon ; Maccoss, Malcolm ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(16), pp.2205-2208 [Peer Reviewed Journal]

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Title:
N-Aryl-prolyl-dipeptides as potent antagonists of VLA-4
Author: Kamenecka, Theodore M ; Lanza, Jr, Thomas ; de Laszlo, Stephen E ; Li, Bing ; Mccauley, Ermengilda D ; Van Riper, Gail ; Egger, Linda A ; Kidambi, Usha ; Mumford, Richard A ; Tong, Sharon ; Maccoss, Malcolm ; Schmidt, John A ; Hagmann, William K
Description: The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as small molecule VLA-4 antagonists is described. Potency against VLA-4 and alpha(4)beta(7) and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues.
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(16), pp.2205-2208
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/S0960-894X(02)00356-6
Subjects: Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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