Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists

被引：19

作者：

Chen, L ^{[1
]}

Trilles, R ^{[1
]}

Miklowski, D ^{[1
]}

Huang, TN ^{[1
]}

Fry, D ^{[1
]}

Campbell, R ^{[1
]}

Rowan, K ^{[1
]}

Schwinge, V ^{[1
]}

Tilley, JW ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(02)00201-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists characterized by the N-(alpha-phenylcyclopentanoyl- and the N-(2,6-dimethylbenzoyl)-derivatives 60 and 64. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1679 / 1682

页数：4

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