Citation: Bi LUO, Chu ZHENG, Zhao-Guo HONG, Xiao-Feng WANG, He-Dong BIAN, Fu-Ping HUANG. Synthesis, Characterization and Antibacterial Activities Study of a Pharmaceutical Cocrystal of Artesunate and 4, 4΄-Bipyridine[J]. Chinese Journal of Structural Chemistry, ;2020, 39(9): 1633-1638. doi: 10.14102/j.cnki.0254-5861.2011-2668 shu

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

State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, Guilin 541001, China

Corresponding author: Fu-Ping HUANG, huangfp2010@163.com
Received Date: 18 November 2019
Accepted Date: 18 March 2020

Fund Project: the National Natural Science Foundation of China 21861005the Foundation of Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources CMEMR2018-C15the Foundation of Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources CMEMR2016-A11

Figures(4)

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.
- cocrystal,
- artesunate,
- active pharmaceutical ingredients,
- antimicrobial activities
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