Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists

被引：8
|
作者：
Kopka, IE
Lin, LS
Mumford, RA
Lanza, T
Magriotis, PA
Young, D
DeLaszlo, SE
MacCoss, M
Mills, SG
Van Riper, G
McCauley, E
Lyons, K
Vincent, S
Egger, LA
Kidambi, U
Stearns, R
Colletti, A
Teffera, Y
Tong, S
Owens, K
Levorse, D
Schmidt, JA
Hagmann, WK
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Inflammat & Rheumatol Res, Rahway, NJ 07065 USA
[3] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期
关键词：
D O I：
10.1016/S0960-894X(02)00460-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituted N-(3,5-dichlorobenzenesulfonyl)-(L)-prolyl- and (L)-azetidyl-beta-biaryl beta-alanine derivatives was prepared as selective and potent VLA-4 antagonists. The 2,6-dioxygenated biaryl substitution pattern is important for optimizing potency. Oral bioavailability was variable and may be a result of binding to circulating plasma proteins. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2415 / 2418
页数：4
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