Amidines as amide bond replacements in VLA-4 antagonists

被引：17

作者：

Kamenecka, TM ^{[1
]}

Park, YJ

Lin, LS

de Laszlo, S

McCauley, ED

Van Riper, G

Egger, L

Kidambi, U

Mumford, RA

Tong, S

Tang, W

Colletti, A

Teffera, Y

Stearns, R

MacCross, M

Schmidt, JA

Hagmann, WK

机构：

[1] Merck & Co Inc, Merck Sharp & Dohme Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Merck Sharp & Dohme Res Labs, Dept Inflammat & Rheumatol Res, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Merck Sharp & Dohme Res Labs, Dept Pharmacol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 09期

关键词：

VLA-4; integrin; asthma; inflammation;

D O I：

10.1016/j.bmcl.2004.01.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

VLA-4 (alpha(4)beta(1), very late activating antigen-4), a key cell surface integrin plays an important role in inflammation by promoting leukocyte attachment and extravasation from the vasculature into the peripheral tissues. As such, VLA-4 antagonists may be useful in the treatment, prevention, and suppression of diseases where cell adhesion and migration are important such as asthma, rheumatoid arthritis, and multiple sclerosis. Herein, we report on the discovery, synthesis, and biological evaluation of amidines as small molecule antagonists of VLA-4. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2323 / 2326

页数：4

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