Binder D, Noe C R, Prager B C, Turnowsky F
Arzneimittelforschung. 1983;33(6):803-5.
The synthesis of substituted pteridine-5,8-dioxides (6) via reaction of furoxanes (5) with enolizing carbonyl compounds is described. Compounds 5 are obtained either through reaction of chloro pyrimidines 1 with sodium azide, or through diazotization of hydrazino pyrimidine 2 and subsequent thermal decomposition of 3 or through nucleophilic displacement of methoxy against amino groups in 5. The antibacterial activity of the compounds 6a and 6c is directed against some gramnegative organisms, i.e. E. coli, Klebsiella spp. and Proteus spp., with MIC values and ED50 values which do not exceed those of the corresponding pyridol [2,3-b]pyrazine-1,4-dioxides.
描述了通过呋咱(5)与可烯醇化的羰基化合物反应合成取代的蝶啶-5,8-二氧化物(6)的方法。化合物5可通过氯嘧啶1与叠氮化钠反应制得,或通过肼基嘧啶2的重氮化以及随后3的热分解制得,或者通过5中甲氧基被氨基亲核取代制得。化合物6a和6c对一些革兰氏阴性菌具有抗菌活性,即大肠杆菌、克雷伯氏菌属和变形杆菌属,其MIC值和ED50值不超过相应的吡啶并[2,3-b]吡嗪-1,4-二氧化物。