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1
Selective chiral inhibitors of 5-lipoxygenase with anti-inflammatory activity.具有抗炎活性的5-脂氧合酶选择性手性抑制剂。
Br J Pharmacol. 1990 Nov;101(3):501-3. doi: 10.1111/j.1476-5381.1990.tb14111.x.
2
(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity.
J Med Chem. 1991 Jul;34(7):2176-86. doi: 10.1021/jm00111a038.
3
Methoxyalkyl thiazoles: a novel series of potent, orally active and enantioselective inhibitors of 5-lipoxygenase.
Agents Actions. 1991 Sep;34(1-2):110-2. doi: 10.1007/BF01993252.
4
2-substituted indazolinones: orally active and selective 5-lipoxygenase inhibitors with anti-inflammatory activity.2-取代吲唑啉酮：具有抗炎活性的口服活性且选择性的5-脂氧合酶抑制剂。
Br J Pharmacol. 1990 Jan;99(1):113-8. doi: 10.1111/j.1476-5381.1990.tb14663.x.
5
Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors.
J Med Chem. 1992 Jul 10;35(14):2600-9. doi: 10.1021/jm00092a010.
6
Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase.ICI D2138的临床前药理学，一种强效口服活性5-脂氧合酶非氧化还原抑制剂。
Br J Pharmacol. 1992 Dec;107(4):1042-7. doi: 10.1111/j.1476-5381.1992.tb13404.x.
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Identification of 4-[4-(4-fluoro-phenyl)-thiazol-2-ylamino]-2,6-dimethyl-phenol (KR-33749) as an inhibitor of 5-lipoxygenase with potent antiinflammatory activity.鉴定出 4-[4-(4-氟苯基)-噻唑-2-基氨基]-2,6-二甲基苯酚（KR-33749）是一种具有强效抗炎活性的 5-脂氧合酶抑制剂。
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Evaluation of the antiinflammatory activity of a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitor, RWJ 63556, in a canine model of inflammation.在犬类炎症模型中对双环氧化酶-2选择性/5-脂氧合酶抑制剂RWJ 63556的抗炎活性进行评估。
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Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton.一种强效、选择性白三烯A4水解酶抑制剂与5-脂氧合酶抑制剂齐留通相比的抗炎活性。
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引用本文的文献

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Design and Synthesis of New Benzophenone Derivatives with In Vivo Anti-Inflammatory Activity through Dual Inhibition of Edema and Neutrophil Recruitment.新型苯甲酮衍生物的设计与合成及其体内抗炎活性研究——通过双重抑制水肿和中性粒细胞募集
Molecules. 2018 Jul 26;23(8):1859. doi: 10.3390/molecules23081859.
2
Pharmacological inhibition of leukotriene actions.白三烯作用的药理学抑制
Pharm World Sci. 1998 Apr;20(2):60-5. doi: 10.1023/a:1008698027211.
3
Specific inhibition of leukotriene B4 (LTB4)-induced neutrophil emigration by 20-hydroxy LTB4: implications for the regulation of inflammatory responses.20-羟基白三烯B4对白三烯B4诱导的中性粒细胞迁移的特异性抑制作用：对炎症反应调节的意义
Br J Pharmacol. 1993 Sep;110(1):423-7. doi: 10.1111/j.1476-5381.1993.tb13827.x.
4
Effect of the 5-lipoxygenase inhibitor ZD2138 on allergen-induced early and late asthmatic responses.5-脂氧合酶抑制剂ZD2138对变应原诱导的哮喘早发和迟发反应的影响。
Thorax. 1994 Aug;49(8):743-8. doi: 10.1136/thx.49.8.743.
5
Lipoxygenase inhibitory activity of U-66,858 and its deacetylated metabolite U-68,244 in human whole blood.U-66,858及其脱乙酰代谢物U-68,244在人全血中的脂氧合酶抑制活性。
Agents Actions. 1994 Mar;41(1-2):32-6. doi: 10.1007/BF01986390.
6
Methoxyalkyl thiazoles: a novel series of potent, orally active and enantioselective inhibitors of 5-lipoxygenase.
Agents Actions. 1991 Sep;34(1-2):110-2. doi: 10.1007/BF01993252.
7
Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase.ICI D2138的临床前药理学，一种强效口服活性5-脂氧合酶非氧化还原抑制剂。
Br J Pharmacol. 1992 Dec;107(4):1042-7. doi: 10.1111/j.1476-5381.1992.tb13404.x.

本文引用的文献

1
Relationship between inhibition of prostaglandin synthesis and drug efficacy: support for the current theory on mode of action of aspirin-like drugs.前列腺素合成抑制与药物疗效之间的关系：对当前阿司匹林类药物作用模式理论的支持。
Biochem Biophys Res Commun. 1972 Jan 31;46(2):552-9. doi: 10.1016/s0006-291x(72)80174-8.
2
Kinetic mechanism of guinea pig neutrophil 5-lipoxygenase.豚鼠中性粒细胞5-脂氧合酶的动力学机制
J Biol Chem. 1986 Sep 5;261(25):11512-9.
3
Selective inhibition of arachidonate 5-lipoxygenase by novel acetohydroxamic acids: biochemical assessment in vitro and ex vivo.新型乙酰氧肟酸对花生四烯酸5-脂氧合酶的选择性抑制：体外和体内生化评估
Br J Pharmacol. 1988 Jun;94(2):528-39. doi: 10.1111/j.1476-5381.1988.tb11557.x.
4
Leukotriene B4 and prostaglandin E2 mediate the inflammatory response of rabbit skin to intradermal arachidonic acid.白三烯B4和前列腺素E2介导兔皮肤对皮内注射花生四烯酸的炎症反应。
Br J Pharmacol. 1987 Nov;92(3):545-52. doi: 10.1111/j.1476-5381.1987.tb11355.x.
5
2-substituted indazolinones: orally active and selective 5-lipoxygenase inhibitors with anti-inflammatory activity.2-取代吲唑啉酮：具有抗炎活性的口服活性且选择性的5-脂氧合酶抑制剂。
Br J Pharmacol. 1990 Jan;99(1):113-8. doi: 10.1111/j.1476-5381.1990.tb14663.x.

具有抗炎活性的5-脂氧合酶选择性手性抑制剂。

Selective chiral inhibitors of 5-lipoxygenase with anti-inflammatory activity.

作者信息

McMillan R M, Girodeau J M, Foster S J

机构信息

Bioscience 1, ICI Pharmaceuticals, Macclesfield, Cheshire.

出版信息

Br J Pharmacol. 1990 Nov;101(3):501-3. doi: 10.1111/j.1476-5381.1990.tb14111.x.

DOI:10.1111/j.1476-5381.1990.tb14111.x
PMID:1963796
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1917719/
Abstract

The studies described here, using enantiomers of an optically-active methoxy alkyl thiazole ICI216800 (1-methoxy-6-(naphth-2-yl-methoxyl)-1- (thiazol-2-yl)indane), provide unequivocal evidence for a specific, chiral interaction with 5-lipoxygenase. In accordance with their biochemical efficacy these compounds also demonstrate enantio-specific anti-inflammatory activity in a leukotriene-mediated model of inflammation. This is the first class of compounds for which 5-lipoxygenase inhibition and anti-inflammatory activity have been shown to be mediated via a specific chiral interaction.

摘要

本文所述的研究使用了具有光学活性的甲氧基烷基噻唑ICI216800（1-甲氧基-6-（萘-2-基甲氧基）-1-（噻唑-2-基）茚满）的对映体，为与5-脂氧合酶的特异性手性相互作用提供了明确证据。根据其生化功效，这些化合物在白三烯介导的炎症模型中也表现出对映体特异性抗炎活性。这是第一类被证明5-脂氧合酶抑制和抗炎活性是通过特异性手性相互作用介导的化合物。