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

页码：2415 / 2418

页数：4

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