concentration (MBC) values of the most active compounds were equal to MIC classifying them as bactericidal agents against Gram-negative bacteria. Sixteen compounds among eighteen carbohydrate-based naphthoquinones tested showed no hemolytic effects on health human erythrocytes whereas more susceptibility to hemolytic cleavage was observed when using non-glycoconjugate amino compounds. In silico Absorption
抗生素耐药性已成为一个严重的全球性公共卫生问题,近来很少发现抗生素并将其引入临床实践。因此,迫切需要开发具有新的作用机理的抗菌化合物,尤其是能够逃避已知抗性机理的抗菌化合物。在这项工作中,合成了衍生自
异喹啉5,8-二酮和
1,4-萘醌的两个系列的糖缀合物和非糖缀合物
氨基化合物及其卤代衍
生物,并评估了它们对革兰氏阳性菌(粪肠球菌A
TCC 29212,
金黄色葡萄球菌A
TCC 25923,表皮葡萄球菌A
TCC 12228,模拟葡萄球菌A
TCC 27851)和革兰氏阴性细菌(大肠杆菌A
TCC 25922,奇异变形杆菌ProCC 15290 ,肺炎克雷伯菌A
TCC 4352和
铜绿假单胞菌(A
TCC 27853)具有临床重要性的菌株。这项研究表明,衍生自卤代
萘醌的糖缀合物对革兰氏阴性菌株更具活性,据文献报道,这种菌株导致感染的治疗更加困难。在临床和实验室标准协会的MIC值(CLSI为0.08-256μg/