Abstract
AbstractNovelty: Novel benzenesulfonamide derivatives are claimed for the treatment of leukotriene mediated disorders with a process for their preparation. They are potentially useful for the treatment of allergic conditions such as psoriasis, asthma, cardiovascular and cerebrovascular disorders and inflammatory and arthritic conditions.Biology: 5LPO inhibition was measured by the method of Carey et ul. (Prosruglandins, Leukotriene Med. (1986) 2257) and the specified compound gave an IC50 value of 1 pM against LTB4. An ex vivo variation of this test using rats is described but no specific results are presented. In vivo the effect of the compound on LTB4 liberation induced in rats by zymosan was measured. The specified compound gave an oral ED50 of 1.5 mgkg against LTB4.Chemistry: Preparation is described in three schemes, exemplified in fifteen cases and forms subsidiary part of the claim. Six compounds are specifically claimed including 4-[3-(4-methoxytetrahydropyran-4-yl)phenylthio]-N-(%-thiazolyl)benzene sulphonamide.
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