有机化学 ›› 2013, Vol. 33 ›› Issue (05): 1074-1079.DOI: 10.6023/cjoc201210020 上一篇    下一篇

研究论文

新型嘧啶并喹啉衍生物的合成及体外抑菌活性评价

陈玉a, 柏舜a, 艾勇b, 范华b, 杨光忠b   

  1. a 中南民族大学化学与材料科学学院 武汉 430074;
    b 中南民族大学药学院 武汉 430074
  • 收稿日期:2012-10-13 修回日期:2012-12-16 发布日期:2013-01-04
  • 通讯作者: 杨光忠,yanggz888@126.com E-mail:yanggz888@126.com
  • 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

Chen Yua, Bai Shuna, Ai Yongb, Fan Huab, Yang Guangzhongb   

  1. a College of Chemistry and Materials Science, South-Central University for Nationalities, Wuhan 430074;
    b College of Pharmacy, South-Central University for Nationalities, Wuhan 430074
  • Received:2012-10-13 Revised:2012-12-16 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

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.

Key words: pyrimidoquinoline derivative, antimicrobial evaluation, azo-Wittig reaction