EUK-418(EUK-418) - 药物靶点：Free radicals_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

Free radicals

作用机制

自由基抑制剂

治疗领域

神经系统疾病内分泌与代谢疾病

在研适应症-

非在研适应症

帕金森病

原研机构

Tyrian Diagnostics Ltd.

在研机构-

非在研机构

Tyrian Diagnostics Ltd.

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 EUK-418 相关的临床结果

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100 项与 EUK-418 相关的转化医学

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100 项与 EUK-418 相关的专利（医药）

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1

项与 EUK-418 相关的文献（医药）

2009-08-01·JBIC Journal of Biological Inorganic Chemistry3区 · 化学

Orally available Mn porphyrins with superoxide dismutase and catalase activities

3区 · 化学

Article

作者: Wyeth B. Callaway ; Karl D. Huffman ; Rosalind A. Rosenthal ; Leslie W. Fisette ; Christy A. Damphousse ; Bernard Malfroy ; Susan R. Doctrow

Superoxide dismutase/catalase mimetics, such as salen Mn complexes and certain metalloporphyrins, catalytically neutralize reactive oxygen and nitrogen species, which have been implicated in the pathogenesis of many serious diseases. Both classes of mimetic are protective in animal models of oxidative stress. However, only AEOL11207 and EUK-418, two uncharged Mn porphyrins, have been shown to be orally bioavailable. In this study, EUK-418 and several new analogs (the EUK-400 series) were synthesized and shown to exhibit superoxide dismutase, catalase, and peroxidase activities in vitro. Some also protected PC12 cells against staurosporine-induced cell death. All EUK-400 compounds were stable in simulated gastric fluid, and most were substantially more lipophilic than the salen Mn complexes EUK-189 and EUK-207, which lack oral activity. Pharmacokinetics studies demonstrate the presence of all EUK-400 series compounds in the plasma of rats after oral administration. These EUK-400 series compounds are potential oral therapeutic agents for cellular damage caused by oxidative stress.

100 项与 EUK-418 相关的药物交易

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