Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University)(Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University))

概要

基本信息

药物类型

小分子化药

别名-

靶点

5-LOX x PGES

作用机制

5-LOX抑制剂(5-脂氧合酶抑制剂)、PGES抑制剂(前列腺素E合成酶抑制剂)

治疗领域

其他疾病

在研适应症

炎症

非在研适应症-

原研机构

Eberhard Karls Universität Tübingen

在研机构

Eberhard Karls Universität Tübingen

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University) 相关的临床结果

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100 项与 Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University) 相关的转化医学

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100 项与 Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University) 相关的专利（医药）

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1

项与 Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University) 相关的文献（医药）

2012-10-25·Journal of medicinal chemistry1区 · 医学

Modified Acidic Nonsteroidal Anti-Inflammatory Drugs as Dual Inhibitors of mPGES-1 and 5-LOX

1区 · 医学

Article

作者: Werz, Oliver ; Laufer, Stefan A. ; Ambrosi, Giulia ; Elkady, Mahmoud ; Bauer, Julia ; Luderer, Susann ; Schaible, Anja M. ; Nieß, Raimund

mPGES-1 is a promising target for development of new anti-inflammatory drugs. We aimed to create mPGES-1 inhibitors by modifying the structure of NSAIDs by replacing the carboxylic acid functionality by sulfonamide moieties. Compounds were also tested for 5-LOX inhibition. The most potent mPGES-1 inhibitor was lonazolac derivative 22 (IC₅₀ = 0.16 μM), while the best 5-LOX inhibition was attained by indomethacin derivative 17 (IC₅₀ = 0.9 μM). Inhibition of COX-1 activity was completely removed.

100 项与 Dual inhibitors of mPGES-1 and 5-LOX(Eberhard Karls University) 相关的药物交易

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