Leukotriene receptor antagonists. 1. Synthesis and structure-activity relationships of alkoxyacetophenone derivatives

…, GJ Cullinan, D Swanson-Bean…

文献索引：Marshall; Goodson; Cullinan; Swanson-Bean; Haisch; Rinkema; Fleisch Journal of Medicinal Chemistry, 1987 , vol. 30, # 4 p. 682 - 689

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被引用次数: 62

摘要

A series of derivatives of 2, 4-dihydroxy-3-propylacetophenone (1) were prepared and examined for their ability to block leukotriene D4 (LTD4) induced contraction of guinea pig ileum. Straight-chain carboxylic acids where the carboxyl group was separated from the acetophenone moiety by varying numbers of methylenes were evaluated, and maximum activity was obtained with the pentamethylene acid (6). Examination of ring substitution ...