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Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase. 1993
G C Crawley, and
T G Bird, and
P Bruneau, and
R I Dowell, and
P N Edwards, and
S J Foster, and
J M Girodeau, and
R M McMillan, and
E R Walker, and
D Waterson
Research Department 1, ICI Pharmaceuticals, Alderley Park, Macclesfield, UK.
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.
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