N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists

被引：38

作者：

Chen, L ^{[1
]}

Tilley, JW ^{[1
]}

Guthrie, RW ^{[1
]}

Mennona, F ^{[1
]}

Huang, TN ^{[1
]}

Kaplan, G ^{[1
]}

Trilles, R ^{[1
]}

Miklowski, D ^{[1
]}

Huby, N ^{[1
]}

Schwinge, V ^{[1
]}

Wolitzky, B ^{[1
]}

Rowan, K ^{[1
]}

机构：

[1] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)00089-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA assay and low-mu M activity in a cell based assay. (C) 2000 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：729 / 733

页数：5

共 8 条

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