申请人:SMITHKLINE BEECHAM CORPORATION
公开号:EP0203787A2
公开(公告)日:1986-12-03
6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-di- hydroimidazo-[2,1-b]thiazoles and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-blthiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.
6-芳基-2,3-二氢咪唑并[2,1-b]噻唑和相应的噻嗪作为亲核体,直接或以格氏试剂的形式与 N-酰基吡啶鎓盐作用,生成新的 6-芳基-5-(N-酰基-1,4-二氢-4-吡啶基)-2,3-二氢咪唑并[2,1-b]噻唑和相应的噻嗪。这些物质经氧化后可得到相应的吡啶基取代咪唑并[2,1-b]噻唑和噻嗪,它们作为花生四烯酸代谢途径中 5-脂氧合酶的抑制剂具有活性。