Key Laboratory of Drug-Targeting and Drug-Delivery Systems of Ministry of Education, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan 610041, PR China.
Bioorg Med Chem Lett. 2012 Dec 15;22(24):7688-92. doi: 10.1016/j.bmcl.2012.09.106. Epub 2012 Oct 5.
New quinolone derivatives bearing a cis- or trans-cyclohexane side chain at the C-7 position have been synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa using the agar dilution method. The activities of compound 53 against these three bacteria were superior to those of the reference drug lomefloxacin. Compounds bearing a cis-cyclohexane side chain generally exhibited greater antibacterial activity than their corresponding trans-isomers.
已经合成了带有顺式或反式环己烷侧链的新型喹诺酮衍生物，并采用琼脂稀释法评估了它们对金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌的抗菌活性。化合物 53 对这三种细菌的活性优于对照药物洛美沙星。带有顺式环己烷侧链的化合物通常比相应的反式异构体具有更强的抗菌活性。
