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 de...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.展开更多
基金supported by the National Natural Science Foundation of China(No.21861005)the Foundation of Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources(CMEMR2018-C15 and CMEMR2016-A11)。
文摘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.
