Synthesis, Characterization and Antibacterial Activities Study of a Pharmaceutical Cocrystal of Artesunate and 4,4΄-Bipyridine

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摘要 We report here a cocrystal with artesunate as the active pharmaceutical ingredient (API) and a pharmaceutical intermediate 4,4΄-bipyridine as the cocrystal former (CCF). The analysis of single-crystal X-ray diffraction demonstrates that the eutectic structural unit consists of two artesunate molecules and one 4,4΄-bipyridine molecule with their ratio to be 2:1. The carboxyl group on artesunate acts as a donor, and the acceptor is N on 4,4΄-bipyridine, forming an O–H···N hydrogen bond. The appearance of new diffraction peaks in the X-ray powder diffraction pattern also indicates the formation of new phases. The PXRD results indicated a pure phase for the synthesized sample. The cocrystal is slightly soluble in water. Antimicrobial activities showed that the cocrystal displayed effective inhibition of different bacteria.

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	罗碧
	郑楚
	洪朝国
	王小凤
	边贺东
	黄富平

关键词 ： cocrystal, artesunate, active pharmaceutical ingredients, antimicrobial activities

Abstract：We report here a cocrystal with artesunate as the active pharmaceutical ingredient (API) and a pharmaceutical intermediate 4,4΄-bipyridine as the cocrystal former (CCF). The analysis of single-crystal X-ray diffraction demonstrates that the eutectic structural unit consists of two artesunate molecules and one 4,4΄-bipyridine molecule with their ratio to be 2:1. The carboxyl group on artesunate acts as a donor, and the acceptor is N on 4,4΄-bipyridine, forming an O–H···N hydrogen bond. The appearance of new diffraction peaks in the X-ray powder diffraction pattern also indicates the formation of new phases. The PXRD results indicated a pure phase for the synthesized sample. The cocrystal is slightly soluble in water. Antimicrobial activities showed that the cocrystal displayed effective inhibition of different bacteria.

Key words： cocrystal artesunate active pharmaceutical ingredients antimicrobial activities

收稿日期: 2019-11-18 出版日期: 2020-09-11

基金资助:The project was supported by the National Natural Science Foundation of China (No. 21861005) and the Foundation of Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (CMEMR2018-C15 and CMEMR2016-A11)

通讯作者: huangfp2010@163.com E-mail: huangfp2010@163.com

引用本文:

罗碧;郑楚;洪朝国;王小凤;边贺东;黄富平. Synthesis, Characterization and Antibacterial Activities Study of a Pharmaceutical Cocrystal of Artesunate and 4,4΄-Bipyridine[J]. 结构化学, 2020, 39(9): 1633-1638.
LUO Bi;ZHENG Chu;HONG Zhao-Guo;WANG Xiao-Feng;BIAN He-Dong;HUANG Fu-Ping. Synthesis, Characterization and Antibacterial Activities Study of a Pharmaceutical Cocrystal of Artesunate and 4,4΄-Bipyridine. CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2020, 39(9): 1633-1638.

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http://manu30.magtech.com.cn/jghx/CN/ 或 http://manu30.magtech.com.cn/jghx/CN/Y2020/V39/I9/1633

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