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

doi:10.6023/cjoc201610016

Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (4): 959-966.DOI: 10.6023/cjoc201610016 Previous Articles Next Articles

ARTICLE

吡啶查尔酮衍生物的合成及抑制耐甲氧西林金黄色葡萄球菌活性评价

张恩^a,b, 王铭铭^a, 徐帅民^a, 王上^a, 赵娣^a, 白鹏燕^a, 崔得运^a, 化永刚^a, 王亚娜^a, 秦上尚^a,b, 刘宏民^a,b

a. 郑州大学药学院药物研究院郑州 450001;
b. 新药创制与药物安全性评价河南省协同创新中心郑州 450001

收稿日期:2016-10-11 修回日期:2016-12-21 发布日期:2016-12-29
通讯作者: 张恩, 秦上尚 E-mail:zhangen@zzu.eud.cn;qinshangshang@126.com
基金资助:
国家自然科学基金（Nos.U1204206，81501782）和河南省教育厅（No.17A350004）资助项目.

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

Received:2016-10-11 Revised:2016-12-21 Published:2016-12-29
Contact: 10.6023/cjoc201610016 E-mail:zhangen@zzu.eud.cn;qinshangshang@126.com
Supported by:
Project supported by the National Natural Science Foundation of China (Nos. U1204206, 81501782) and the Education Department of Henan Province (No. 17A350004).

1. Synthesis and Antibiotic Activity Study of Pyridine Chalcone Derivatives against Methicillin-Resistant Staphylococcus aureus.PDF(7091KB)

Abstract

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.

Key words: pyridine chalcone, methicillin-resistant Staphylococcus aureus, antibiotic activity, hemolytic activity

Cite this article

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]. Chin. J. Org. Chem., 2017, 37(4): 959-966.

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吡啶查尔酮衍生物的合成及抑制耐甲氧西林金黄色葡萄球菌活性评价

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

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