Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors

被引：32

作者：

Patman, Joanne ^{[1
]}

Bhardwaj, Namrta ^{[1
]}

Ramnauth, Jailall ^{[1
]}

Annedi, Subhash C. ^{[1
]}

Renton, Paul ^{[1
]}

Maddaford, Shawn P. ^{[1
]}

Rakhit, Suman ^{[1
]}

Andrews, John S. ^{[1
]}

机构：

[1] NeurAxon Inc, Mississauga, ON L5J 2Z1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 09期

关键词：

nitric oxide synthase; nitric oxide; inhibitor; 2-aminobenzothiazole;

D O I：

10.1016/j.bmcl.2007.02.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted 2-aminobenzothiazole compounds have been synthesized and evaluated as nitric oxide synthase (NOS) inhibitors. Compound 14 shows activity in the nM range and is selective for the human neuronal NOS isoform. We have also evaluated the compounds against the rat NOS isoforms. For some of the compounds, there are significant differences in NOS inhibitory activities between the human and rat enzymes. For example, compound 10b has nM activity against the rat nNOS while low mu M activity against the human nNOS. (c) 2007 Elsevier Ltd. All rights reserved.

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收藏

页码：2540 / 2544

页数：5

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