N-Acylhydrazones as inhibitors of PDE10A

被引：35

作者：

Gage, Jennifer L. ^{[1
]}

Onrust, Rene ^{[1
]}

Johnston, Derek ^{[2
]}

Osnowski, Andrew ^{[2
]}

MacDonald, Wendy ^{[2
]}

Mitchell, Lee ^{[2
]}

Ueroegdi, Laszlo ^{[3
]}

Rohde, Alex ^{[1
]}

Harbol, Kevin ^{[1
]}

Gragerov, Sasha ^{[1
]}

Dorman, Gyoergy ^{[3
]}

Wheeler, Tom ^{[1
]}

Florio, Vince ^{[1
]}

Cutshall, Neil S. ^{[1
]}

机构：

[1] Omeros Corp, Seattle, WA 98101 USA

[2] Scottish Biomed, Glasgow, Lanark, Scotland

[3] AMRI Hungary Zrt, H-1031 Budapest, Hungary

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 14期

关键词：

PDE10; PDE10A; Phosphodiesterase; Schizophrenia; Hydrazide; PDE; Enzyme inhibitor; Hydrazone; Acylhydrazone; HYDRAZIDE DERIVATIVES; PHOSPHODIESTERASES; ANTAGONISTS; DISCOVERY; ACID; TARGETS;

D O I：

10.1016/j.bmcl.2011.05.100

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Cyclic nucleotide phosphodiesterases (PDEs) are represented by a large superfamily of enzymes. A series of hydrazone-based inhibitors was synthesized and shown to be novel, potent, and selective against PDE10A. Optimized compounds of this class were efficacious in animal models of schizophrenia and may be useful for the treatment of this disease. (C) 2011 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4155 / 4159

页数：5

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