导致发现ICI D2138（一种5-脂氧合酶的选择性、强效且口服活性抑制剂）的结构与活性关系。
Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase.
作者信息
Crawley G C, Bird T G, Bruneau P, Dowell R I, Edwards P N, Foster S J, Girodeau J M, McMillan R M, Walker E R, Waterson D
机构信息
Research Department 1, ICI Pharmaceuticals, Alderley Park, Macclesfield, UK.
出版信息
J Lipid Mediat. 1993 Mar-Apr;6(1-3):249-57.
PMID:8395247
Abstract
Structure and activity relationships of (methoxyalkyl)thiazole and 4-methoxytetrahydropyran series of 5-lipoxygenase inhibitors are reviewed. One member of the 4-methoxytetrahydropyran series, 6-([fluoro-5-(4-methoxy-3,4,5,6-tetrahydro-2H-pyran-4-yl)phenoxy]methyl) -1- methylquinol-2-one (ICI D2138), is undergoing clinical evaluation.
摘要
综述了（甲氧基烷基）噻唑和4-甲氧基四氢吡喃系列5-脂氧合酶抑制剂的结构与活性关系。4-甲氧基四氢吡喃系列的一个成员，6 - （[氟 - 5 - （4 - 甲氧基 - 3,4,5,6 - 四氢 - 2H - 吡喃 - 4 - 基）苯氧基]甲基）-1 - 甲基喹啉 - 2 - 酮（ICI D2138）正在进行临床评估。
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