Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

被引：27

作者：

Debenham, JS

Madsen-Duggan, CB

Walsh, TF

Wang, JY

Tong, XC

Doss, GA

Lao, J

Fong, TM

Schaeffer, MT

Xiao, JC

Huang, CRRC

Shen, CP

Feng, Y

Marsh, DJ

Stribling, DS

Shearman, LP

Strack, AM

MacIntyre, DE

Van der Ploeg, LHT

Goulet, MT

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Pharmacol, Rahway, NJ 07065 USA

[5] Merck Res Labs, Boston, MA 02115 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 03期

关键词：

cannabinoid; CB1; inverse agonist; anorexigenic; obesity; CB2;

D O I：

10.1016/j.bmcl.2005.10.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis, SAR, and binding affinities are described for a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists. Food intake, knockout mouse, and pharmacokinetic evaluation of 14 indicate that this compound is an effective orally active modulator of CB1. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：681 / 685

页数：5

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