Citation: Gao Zhimin, Wang Tiantian, Li Shenzhen, Wan Huiqi, Wang Gang, Wu Yinbin, Deng Xianqing, Song Mingxia. Synthesis and Antibacterial Activity Evaluation of (2-Chloroquinolin- 3-yl)methyleneamino Guanidine Derivatives[J]. Chinese Journal of Organic Chemistry, ;2016, 36(10): 2484-2488. doi: 10.6023/cjoc201604041 shu

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

1.
Basic Medical and Pharmacy College, Jinggangshan University, Ji'an 343009

Corresponding author: Song Mingxia, freexiaoxiao83@aliyun.com
Received Date: 19 April 2016
Revised Date: 31 May 2016

Fund Project: National Natural Science Foundation of China 81560561Doctoral Foundation of Jinggangshan University JZB1317

Figures(1)

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.
- alkylene aminoguanidine,
- 2-chloroquinoline,
- antibacterial activity,
- drug-resistance bacteria
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沈阳化工大学材料科学与工程学院沈阳 110142