Citation: Zhang En, Wang Mingming, Xu Shuaimin, Wang Shang, Zhao Di, Bai Pengyan, Cui Deyun, Hua Yonggang, Wang Ya'na, Qin Shangshang, Liu Hongmin. Synthesis and Antibiotic Activity Study of Pyridine Chalcone Derivatives against Methicillin-Resistant Staphylococcus aureus[J]. Chinese Journal of Organic Chemistry, ;2017, 37(4): 959-966. doi: 10.6023/cjoc201610016 shu

Synthesis and Antibiotic Activity Study of Pyridine Chalcone Derivatives against Methicillin-Resistant Staphylococcus aureus

Zhang En ^a,b,*,, ,
Wang Mingming ^a ,
Xu Shuaimin ^a ,
Wang Shang ^a ,
Zhao Di ^a ,
Bai Pengyan ^a ,
Cui Deyun ^a ,
Hua Yonggang ^a ,
Wang Ya'na ^a ,
Qin Shangshang ^a,b,*,, ,
Liu Hongmin ^a,b

a.
Institute of Drug Discovery and Development, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
b.
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Zhengzhou 450001

Corresponding author: Zhang En, zhangen@zzu.eud.cn Qin Shangshang, qinshangshang@126.com
Received Date: 11 October 2016
Revised Date: 21 December 2016

Fund Project: the National Natural Science Foundation of China U1204206the National Natural Science Foundation of China 81501782the Education Department of Henan Province 17A350004

Figures(3)

A series of pyridine chalcone derivatives were designed and synthesized. The structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. In vitro biological activity evaluation results showed that five of the compounds exhibited good biological activity against gram positive bacteria staphylococcus aureus (ATCC 29213). Further antibiotic activity of these five compounds against 11 clinical isolated methicillin-resistant staphylococcus aureus (MRSA) were evaluated. The results showed that four of the compounds exhibited good antibacterial activity against MRSA. (E)-2-Bromo-N-{4-[3-(pyridin-2-yl)-acryloyl]phenyl}acetamide (5k) showed the most effective activity (minimum inhibitory concentration, MIC=4 μg/mL). In terms of hemolytic activity evaluation, compound 5k showed virtually no toxicity even in 1000 μg/mL concentration. To sum up, pyridine chalcone 5k was potential for further antibiotic study as anti-MRSA agent.
- pyridine chalcone,
- methicillin-resistant Staphylococcus aureus,
- antibiotic activity,
- hemolytic activity
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