有机化学 ›› 2016, Vol. 36 ›› Issue (10): 2484-2488.DOI: 10.6023/cjoc201604041 上一篇    下一篇

研究简报

2-氯喹啉-3-甲醛缩氨基胍衍生物的合成及其抗菌活性评价

高智敏, 王田田, 李深圳, 万慧琪, 王刚, 吴银彬, 邓先清, 宋明霞   

  1. 井冈山大学基础医学与药学学院 吉安 343009
  • 收稿日期:2016-04-19 修回日期:2016-05-31 发布日期:2016-06-08
  • 通讯作者: 宋明霞,E-mail:freexiaoxiao83@aliyun.com E-mail:freexiaoxiao83@aliyun.com
  • 基金资助:

    国家自然科学基金(No.81560561)和井冈山大学博士启动基金(No.JZB1317)资助项目.

Synthesis and Antibacterial Activity Evaluation of (2-Chloroquinolin- 3-yl)methyleneamino Guanidine Derivatives

Gao Zhimin, Wang Tiantian, Li Shenzhen, Wan Huiqi, Wang Gang, Wu Yinbin, Deng Xianqing, Song Mingxia   

  1. Basic Medical and Pharmacy College, Jinggangshan University, Ji'an 343009
  • Received:2016-04-19 Revised:2016-05-31 Published:2016-06-08
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.21562028), and the Doctoral Foundation of Jinggangshan University (No.JZB1317).

为寻找新的高活性的广谱抗菌剂,通过活性拼接原理,设计合成了8个未见文献报道的2-氯喹啉-3-甲醛缩氨基胍衍生物,并通过光谱方法确证结构.所合成化合物对所选的菌种(除了Salmonella typhimurium 2421和Pseudomonas aeruginosa 2742)均显示出了较好的抑制活性,最低抑菌浓度值(MIC)范围大都为2.0~16 μg/mL.化合物4h显示出最好的广谱抗菌活性,其对抗所选的6种菌株的最低抑菌浓度值均为2.0 μg/mL.其对抗Staphylococcus aureus KCTC 503和两种耐药菌(Methicillin-resistant Staphylococcus aureus CCARM 3167和Quinolone-resistant Staphylococcus aureus CCARM 3505)的活性要优于或相当于阳性对照药加替沙星、莫西沙星、诺氟沙星和苯唑西林.

关键词: 缩氨基胍, 2-氯喹啉, 抗菌活性, 耐药菌

In order to find new antibacterial agent with wide spectra and high activities, 8 new (2-chloroquinolin-3-yl)meth- yleneamino guanidine derivatives were synthesized based on combination principles, whose structures were then identified by spectral methods. All of the compounds provided exhibited good inhibitory activities against the strains chosen, except Salmonella typhimurium 2421 and Pseudomonas aeruginosa 2742, of which MICs were mostly in the range of 2.0~16 μg/mL. The compound 4h showed the best broad-spectrum antibacterial activities, whose MIC value was 2.0 μg/mL against six strains. The inhibitory activities of 4h, against Staphylococcus aureus KCTC 503 and two drug-resistance bacterias (Methicillin-resistant Staphylococcus aureus CCARM 3167 and Quinolone-resistant Staphylococcus aureus CCARM 3505), were superior or equal to positive controls gatifloxacin, moxifloxacin, norfloxacin and oxacillin.

Key words: alkylene aminoguanidine, 2-chloroquinoline, antibacterial activity, drug-resistance bacteria