N-[(arylmethoxy) phenyl] and N-[(arylmethoxy) naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure

…, RHW Bender, DM Kubrak, RP Carlson…

文献索引：Musser, John H.; Kreft, Anthony F.; Bender, Reinhold H. W.; Kubrak, Dennis M.; Carlson, Richard P.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1176 - 1183

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被引用次数: 18

摘要

Two series of compounds, N-[(ary1methoxy) phenyll sulfonamides and N-[(ary1methoxy) naphthyll sulfonamides, were prepared as leukotriene D4 (LTD4) antagonists. In the phenyl series, N-[3-(2-quinolinylmethoxy) phenyl]-trifluoromethanesulfonamide (Wy-48,252, 16) was the most potent inhibitor of LTD4-induced bronchoconstriction in the guinea pig. With an intragastric ID50 of 0.1 mg/kg (2-h pretreatment), 16 was 300 times more potent than LY- ...