作者:Walaa Ibraheem、Capucine Chaar、Emilie Camiade、Virginie Hervé、Delphine Fouquenet、Anne-Emmanuelle Roux、Mustapha Si-Tahar、Elhadi Ahmed、Jérôme Thibonnet、Emilie Thiery、Julien Petrignet
DOI:10.1016/j.molstruc.2021.132135
日期:2022.3
history of antibacterial discovery has revealed that natural products, especially secondary metabolites, represent privileged chemical matters for the antibacterial discovery. Among these metabolites, several natural phthalides exhibit interesting antibacterial activities, such as cytosporone E isolated from endophyte ascomycetes Diaporthe and Cytospora sp. We describe herein the synthesis and the pharmacomulations
抗菌发现的历史表明,天然产物,尤其是次级代谢产物,代表了抗菌发现的特殊化学物质。在这些代谢物中,几种天然苯酞表现出令人感兴趣的抗菌活性,例如从内生菌子囊菌Diaporthe和Cytospora sp. 中分离出的胞孢菌素E。我们在此描述了胞孢菌素 E 的 3、4 和 6 位的合成和药物代谢,然后这些化合物对金黄色葡萄球菌包括耐药菌株、大肠杆菌和铜绿假单胞菌的体外抗菌评价. 对最活跃的化合物对人支气管上皮细胞的细胞毒性进行了评估,以检查它们的安全性。