Abstract
SummarySummaryNovelty: Bicyclic pyrans are disclosed as inhibitors of 5-lipoxygenase and are therefore potentially useful in treating leukotriene-mediated diseases such as asthma.Biology: Seven standard test models are outlined with activity ranges defined for the compounds. IC50 values against cyclooxygenase are 20–1000 μM (cf. 1 nM-1 μM against LTC4 synthesis, in the same cells). Specific data are provided for 4-[3-(1,3-dimethyl-2-oxo-2,3-dihydrobenzimidazol-5-ylthio)phenyl]-4-methoxytetrahydropyran, which has an IC50 value of 50 nM against A23187-induced LTB4 synthesis in human whole blood, and an ED50 < 2 mg/kg po in a zymosan-induced LTB4 synthesis, in a rat air pouch model.Chemistry: The compounds are synthesized using conventional methods.Structure:
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