Coburn R A, Carapellotti R A
J Pharm Sci. 1976 Oct;65(10):1505-10. doi: 10.1002/jps.2600651022.
Derivatives of two new and unusual classes of heterocycles, possessing structural similarities to the broad spectrum antibiotic fervenulin, were synthesized and examined for in vitro antimicrobial activity. Only three of 17 mesoionic pyrimido[1,2-b]pyridazine-2,4-diones exhibited evidence of antimicrobial activity while seven of eight mesoionic pyridazino[2,3-a]-s-triazine-2,4-diones were active against one or more microorganisms. Susceptibility toward attack by nucleophiles of both mesoionic pyridazino[2,3-a]-s-triazine-2,4-diones and fervenulin was observed.
合成了两类新型且结构独特的杂环衍生物，它们与广谱抗生素热诚菌素结构相似，并对其进行了体外抗菌活性检测。17种中氮茚并嘧啶并[1,2 - b]哒嗪 - 2,4 - 二酮中只有3种显示出抗菌活性证据，而8种中氮茚并哒嗪并[2,3 - a]-1,3,5 - 三嗪 - 2,4 - 二酮中有7种对一种或多种微生物具有活性。观察到中氮茚并哒嗪并[2,3 - a]-1,3,5 - 三嗪 - 2,4 - 二酮和热诚菌素对亲核试剂攻击的敏感性。
