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

doi:10.6023/cjoc201604041

Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (10): 2484-2488.DOI: 10.6023/cjoc201604041 Previous Articles Next Articles

Notes

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

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

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).

1. Synthesis and Antibacterial Activity Evaluation of (2-Chloroquinolin- 3-yl)methyleneamino Guanidine Derivatives.PDF(2296KB)

Abstract

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

Cite this article

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]. Chin. J. Org. Chem., 2016, 36(10): 2484-2488.

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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

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

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