Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists

被引：31

作者：

Liu, B ^{[1
]}

Liu, G ^{[1
]}

Xin, ZL ^{[1
]}

Serby, MD ^{[1
]}

Zhao, HY ^{[1
]}

Schaefer, VG ^{[1
]}

Falls, HD ^{[1
]}

Kaszubska, W ^{[1
]}

Collins, CA ^{[1
]}

Sham, HL ^{[1
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Metab Dis Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

关键词：

growth hormone secretagogue receptor; ghrelin; antagonist;

D O I：

10.1016/j.bmcl.2004.06.060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel isoxazole carboxamides have been identified as growth hormone secretagogue receptor (GHS-R) antagonists. Substituent modification off the 5-position of the isoxazole ring led to analogues with potent binding affinity and functional antagonism of GHS-R. A potent analogue (32) with high aqueous solubility and good GPCR selectivity was also identified as a potential pharmacological tool for in vivo studies. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5223 / 5226

页数：4

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