小檗碱衍生物的合成及抗菌活性研究OACSTPCD
Synthesis and Antibacterial Activity of Berberine Derivatives
小檗碱具有广谱抗菌活性,但抑菌效果不强.本文对小檗碱进行结构改造,获得了具有更高抗菌活性的小檗碱衍生物.将经典的FtsZ(Filamenting temperature-sensitive mutant Z)抑制剂PC190723衍生物的苯并噻唑类活性片段引入到小檗碱中,对小檗碱进行结构改造并对其进行体外抗菌活性实验.合成出了10个小檗碱衍生物,其中有5个化合物对金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌的抗菌活性明显优于小檗碱.
Berberine has broad-spectrum antibacterial activity,but its antibacterial effect is not very good.The structure of berberine was modified to obtain berberine derivatives with higher antibacterial activity.The active benzothiazoles of PC190723 derivatives,a classical FtsZ inhibitor,were introduced into berberine,and the structure of berberine was modified and its antibacterial activity was tested in vitro.Ten berberine derivatives were synthesized,among which 5 compounds showed significantly bet-ter antibacterial activity against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus.
葛莲;程珊;吕钦;万升标
中国海洋大学医药学院,海洋药物教育部重点实验室,山东 青岛 266003||青岛海洋科学与技术试点国家实验室 海洋药物与生物制品功能实验室,山东 青岛 266237
药学
小檗碱苯并噻唑FtsZ抑制剂结构改造抗菌活性
berberinebenzothiazoleftsz inhibitorstructural modificationantibacterial activity
《中国海洋大学学报（自然科学版）》 2024 (002)
NDM-1金属β-内酰胺酶抑制剂的设计、合成和抗NDM-1耐药菌活性研究
106-113 / 8
国家自然科学基金项目(81973170)资助Supported by the National Natural Science Foundation of China(81973170)
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