N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists

被引：13

作者：

Li, B ^{[1
]}

de Laszlo, SE

Kamenecka, TM

Kopka, IE

Durette, PL

Lanza, T

MacCoss, M

Tong, S

Mumford, RA

McCauley, ED

Van Riper, G

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(02)00366-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4 antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further optimization led to several highly potent compounds (IC50 < 1 nM). Evaluation of rat pharmacokinetic revealed generally high clearance. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2141 / 2144

页数：4

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