Arylthio analogs of 5,8-quinolinedione: Synthesis, characterization, antibacterial, and antifungal evaluations
作者:Hatice Yildirim
DOI:10.1080/10426507.2020.1723097
日期:2020.6.2
vitro antimicrobial effect. The antibacterial and antifungal activities of 6,7-bis(arylthio)-5,8-quinolinedione (4a–f) and 6,7-bis(arylthio)-2-methyl-5,8-quinolinedione (5a–f) were evaluated against four gram-negative bacteria, three gram-positive bacteria, and three fungi strains. The bis(methoxyarylthio) 5,8-quinolinedione analogs presented better activity against especially gram-positive bacteria compared
摘要 合成了一组双(芳硫基)取代的 5,8-喹啉二酮衍生物并研究了它们的体外抗菌作用。6,7-双(芳硫基)-5,8-喹啉二酮(4a-f)和6,7-双(芳硫基)-2-甲基-5,8-喹啉二酮(5a-f)的抗菌和抗真菌活性为对四种革兰氏阴性菌、三种革兰氏阳性菌和三种真菌菌株进行了评估。与双(卤代芳硫基) 5,8-喹啉二酮类似物相比,双(甲氧基芳硫基) 5,8-喹啉二酮类似物表现出更好的抗革兰氏阳性菌活性。双(3-甲氧基芳硫基) 5,8-喹啉二酮 (4e) 对金黄色葡萄球菌具有与参考药物相同的活性。双(2-甲氧基芳硫基) 5,8-喹啉二酮 (4f) 对粪肠球菌的活性提高了两倍半,为 89.69 μM,11.20 μM 对表皮葡萄球菌的活性提高两倍。双(2-甲氧基芳硫基)-2-甲基-5,8-喹啉二酮 5f 的抗菌活性高出五倍,对粪肠球菌的抗菌活性为 43.44 μM,对表皮葡萄球菌的抗菌活性为 2.71