Benzo-and pyrido-1, 4-oxazepin-5-ones and-thiones: synthesis and structure-activity relationships of a new series of H1-antihistamines

…, WJ Welstead Jr, LW Jaques, AF Johnson…

文献索引：Cale Jr.; Gero; Walker; Lo; Welstead Jr.; Jaques; Johnson; Leonard; Nolan Journal of Medicinal Chemistry, 1989 , vol. 32, # 9 p. 2178 - 2199

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被引用次数: 40

摘要

A series of novel benzo-and pyridel, 4-oxazepinones and-thiones which represents a new structural class of compounds possessing H1 antihistaminic activity was synthesized, and the SARs were evaluated. The antihistaminic activity was determined by blockade of histamine-induced lethality in guinea pigs. The sedative potential was determined by comparison of the EEG profiles of the compounds with those of known sedating and ...