茶碱是一种有效的支气管扩张剂,但能引起恶心、呕吐甚至对心血管与中枢神经方面的副作用。作者注意到8-氮杂茶碱对抑制大鼠的被动皮肤过敏试验(PCA)的活性比茶碱强得多,对8-氮杂嘌呤-6-酮母核的改造得到的(2)是一种强力抗变应刻。作者合成一系列的咪唑并[1,2-a]嘌呤-9-(4H)-酮(3)衍生物,发现化合物 Theophylline is an effective bronchodilator, but can cause nausea, vomiting and even cardiovascular and central nervous side effects. The authors note that 8-azithophylline is much more potent than theophylline in inhibiting passive cutaneous anaphylaxis (PCA) in rats and that (2) obtained from the modification of 8-azapurine-6-one A strong anti-change should be engraved. The authors synthesized a series of imidazo [1,2-a] purin-9- (4H) -one (3) derivatives and found that the compound