Schwender C F, Sunday B R, Herzig D J, Kusner E K, Schumann P R, Gawlak D L
J Med Chem. 1979 Jun;22(6):748-50. doi: 10.1021/jm00192a027.
A series of substituted 11-oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acids were prepared and evaluated as antiallergy agents. Several analogues were orally active. 2-Methyl-11-oxo-11H-pyrido[2,1-b]quinoazoline-8-carboxylic acid (6) was superior to cromolyn sodium and doxantrazole orally and intravenously in the rat PCA test and a rat allergic bronchospasm model.
制备了一系列取代的11-氧代-11H-吡啶并[2,1-b]喹唑啉-8-羧酸,并将其作为抗过敏剂进行评估。几种类似物具有口服活性。在大鼠PCA试验和大鼠过敏性支气管痉挛模型中,2-甲基-11-氧代-11H-吡啶并[2,1-b]喹唑啉-8-羧酸(6)在口服和静脉给药时均优于色甘酸钠和多沙唑嗪。