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5-硝基呋喃环的2位上导入杂环后常用作抗菌剂。在此二个杂环之间引入共轭双键,结果可提高在体内的活性。鉴此,过去曾合成了硝基呋喃乙烯基-1,8-萘啶酸的衍生物(Ⅰ),发现具有显著的抗绿脓杆菌和变形杆菌的作用。本文继续合成了一系列5-羟基-2-[2-(5-硝基-2-呋喃)乙烯基]吡啶并[2,3,-d]嘧啶-6-羧酸衍生物(Ⅱ),经筛选结果发现同样有广谱杀菌作用,特别体外试验对革兰氏阳性及革兰氏阴性菌均有高度对抗作用,值得注意的是,其中某些衍生物也具有抗绿脓杆菌及变形杆菌的作用,如果将硝基呋喃乙烯基改为苯乙烯基则减少其抗菌活性。
The introduction of heterocycles at the 2-position of the 5-nitrofuran ring is often used as an antibacterial agent. The introduction of a conjugated double bond between these two heterocycles results in increased in vivo activity. In view of the above, the derivative (I) of nitrofurylvinyl-1,8-nalidixic acid has been synthesized in the past and found to have significant anti-Pseudomonas aeruginosa and proteus. In this paper, we continue to synthesize a series of 5-hydroxy-2- [2- (5-nitro-2-furan) vinyl] pyrido [2,3- d] pyrimidine- The screening results also found broad-spectrum bactericidal effect, in particular, in vitro tests against Gram-positive and Gram-negative bacteria are highly antagonistic effect, it is noteworthy that some of these derivatives also have anti-Pseudomonas aeruginosa and Proteus Role, if the nitrofuryl vinyl to styryl reduced their antimicrobial activity.