Synthesis and antimicrobial activity of chromone-linked 2-pyridone fused with 1,2,4-triazoles, 1,2,4-triazines and 1,2,4-triazepines ring systems
Synthesis and antimicrobial activity of chromone-linked 2-pyridone fused with 1,2,4-triazoles, 1,2,4-triazines and 1,2,4-triazepines ring systems
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DOI：
10.1590/s0103-50532010000600010
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发表时间：
2010-01-01
影响因子：
1.4
通讯作者：
Ibrahim, Magdy Ahmed
中科院分区：
文献类型：
--
作者：
Ali, Tarik El-Sayed;Ibrahim, Magdy Ahmed
以关键中间体1，6-diamino-(6-chloro-4-oxo-4H-chromen-3-yl)-2-oxo-1，2-dihydropyridine-3，5-dicarbonitrile(4)为原料，与亲电试剂反应，合成了1，2，4-三氮唑并[1，5-a]吡啶(5-7和9)、吡啶并[1，2-b][1，2，4]三嗪(10，11，13和15)和吡啶并[1，2-b][1，2，4]三氮杂环(17，18，20和22)等三个新型稠氮杂环体系。通过元素分析和波谱数据确定了新化合物的结构。所有产品还进行了体外抗菌活性筛选。与参比药物相比，化合物7、9和15的活性最高。
Three series of novel fused nitrogen heterocyclic systems such as 1,2,4-triazolo[1,5-a] pyridines (5-7 and 9), pyrido[1,2-b][1,2,4] triazines (10, 11, 13 and 15), and pyrido[1,2-b][1,2,4]triazepines (17, 18, 20 and 22) linked with a chromone moiety were synthesized from the key intermediate 1,6-diamino-(6-chloro-4-oxo-4H-chromen-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile (4) with some electrophilic reagents. The structures of the novel compounds were established by elemental analyses and spectral data. All the products were also screened in vitro for their antimicrobial activity. Compounds 7, 9 and 15 showed the highest activities when compared with the reference drugs.