Substituted isoquinolines and quinazolines as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor α

…, H Shih, LM Leoni, D Genini, DA Carson…

文献索引：Chao, Qi; Deng, Lynn; Shih, Hsiencheng; Leoni, Lorenzo M.; Genini, Davide; Carson, Dennis A.; Cottam, Howard B. Journal of Medicinal Chemistry, 1999 , vol. 42, # 19 p. 3860 - 3873

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被引用次数: 135

摘要

A series of isoquinolin-1-ones and quinazolin-4-ones and related derivatives were prepared and evaluated for their ability to inhibit tumor necrosis factor α (TNFα) production in human peripheral blood monocytes stimulated with bacterial lipopolysaccharide (LPS). In an effort to optimize the TNFα inhibitory activity, a homologous series of N-alkanoic acid esters was prepared. Several electrophilic and nucleophilic substitutions were also carried out. ...