Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists

被引：35

作者：

Vasudevan, A ^{[1
]}

Souers, AJ ^{[1
]}

Freeman, JC ^{[1
]}

Verzal, MK ^{[1
]}

Gao, J ^{[1
]}

Mulhern, MM ^{[1
]}

Wodka, D ^{[1
]}

Lynch, JK ^{[1
]}

Engstrom, KM ^{[1
]}

Wagaw, SH ^{[1
]}

Brodjian, S ^{[1
]}

Dayton, B ^{[1
]}

Falls, DH ^{[1
]}

Bush, E ^{[1
]}

Brune, M ^{[1
]}

Shapiro, RD ^{[1
]}

Marsh, KC ^{[1
]}

Hernandez, LE ^{[1
]}

Collins, CA ^{[1
]}

Kym, PR ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 23期

关键词：

melanin concentrating hormone; obesity; aminoindazoles; palladium amination;

D O I：

10.1016/j.bmcl.2005.08.049

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice. (c) 2005 Published by Elsevier Ltd.

引用

页码：5293 / 5297

页数：5

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