新型嘧啶并喹啉衍生物的合成及体外抑菌活性评价
收稿日期: 2012-10-13
修回日期: 2012-12-16
网络出版日期: 2013-01-04
基金资助
国家科技支撑计划(No. 2012BAI27B06)资助项目.
Synthesis and Antimicrobial Evaluation of Novel Pyrimidoquinolines
Received date: 2012-10-13
Revised date: 2012-12-16
Online published: 2013-01-04
Supported by
Project supported by the National Key Technology R&D Program in the 12th Five Year Plan of China (No. 2012BAI27B06).
采用简便有效的方法合成了一系列新型的嘧啶并[5,4-c]喹啉-4(3H)-酮衍生物, 通过IR, 1H NMR, HRMS对所合成的化合物进行了结构表征, 并用微稀释液体培养法对革兰氏阳性菌(枯草芽孢杆菌和金黄色葡萄球菌)、革兰氏阴性菌(大肠杆菌)以及真菌(白色念珠球菌)进行了体外抑菌活性评价. 抑菌活性的筛选结果表明: 所测化合物均表现一定的抗菌和抗真菌活性.
关键词: 嘧啶并喹啉衍生物; 抑菌评价; 氮杂Wittig反应
陈玉 , 柏舜 , 艾勇 , 范华 , 杨光忠 . 新型嘧啶并喹啉衍生物的合成及体外抑菌活性评价[J]. 有机化学, 2013 , 33(05) : 1074 -1079 . DOI: 10.6023/cjoc201210020
A facile and efficient approach was adopted for the synthesis of a series of novel pyrimido[5,4- c]quinolin-4(3H)-one derivatives. All the synthesized compounds were characterized using spectroscopic data (IR, 1H NMR, and mass spectrometry) and evaluated for their in vitro antimicrobial activities against Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus), Gram-negative bacteria (Escherichia coli) as well as fungi (Canibia albican) by broth microdilution method. The antimicrobial screening revealed that the tested compounds showed slightly to moderate antibacterial and antifungal activities.
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