Citation: Zhang Hong, He Yunhe, Li Yang, Chen Yu. Convenient and Effective Syntheses of Novel 3-Aroxymethylquinoxaline-2-carboxylic acids and Their Antibacterial Activities[J]. Chemistry, ;2020, 83(9): 828-836. shu

Convenient and Effective Syntheses of Novel 3-Aroxymethylquinoxaline-2-carboxylic acids and Their Antibacterial Activities

Zhang Hong ¹ ,
He Yunhe ¹ ,
Li Yang ^1,, ,
Chen Yu ^2,,

1.
College of Chemistry and Chemical Engineering, Bohai University, Jinzhou 121000
2.
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016

Corresponding author: Li Yang, bhuzh@163.com Chen Yu, 569180398@qq.com
Received Date: 29 February 2020
Accepted Date: 8 April 2020

Figures(3)

In the present work, a series of novel 3-aroxymethylquinoxaline-2-carboxylic acids (4a~4l) were synthesized by a simple and facile method using the newly-synthesized ethyl 3-bromomethylquinoxaline-2-carboxylate (6) as substrate through one-pot sequential Williamson reaction with various phenols (8a~8l) followed by ester hydrolysis reaction. A preliminary screening for their in vitro antibacterial activities against five bacterial strains revealed that compounds 4j, 4k and 4l with tert-butyl and halo (F, Cl and Br) substituents exhibited significant activity against Gram (+) bacterials B. subtilis and S. aureus, among them 4j possessed the best activity with the MIC values of 15.625 and 7.8125 μg/mL, respectively, better than the reference drug Ciprofoxacin.
- Quinoxaline,
- Carboxylic acid,
- Williamson reaction,
- One-pot,
- Antibacterial activity
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