Albrecht H A, Beskid G, Christenson J G, Deitcher K H, Georgopapadakou N H, Keith D D, Konzelmann F M, Pruess D L, Wei C C
Roche Research Center, Hoffmann-La Roche Incorporated, Nutley, New Jersey 07110.
J Med Chem. 1994 Feb 4;37(3):400-7. doi: 10.1021/jm00029a012.
We have previously reported that linking quinolones to the cephalosporin 3'-position through an ester bond, a carbamate function, or a bond through a quaternary nitrogen produced cephalosporins with a dual mode of antibacterial action. We now describe a new class of dual-action cephalosporins, with greater chemical stability than those previously reported, in which the basic nitrogen of ciprofloxacin is bonded directly to the 3'-cephalosporin position, i.e., the two moieties are linked through a tertiary amine function. These compounds have demonstrated potent activity against a broad spectrum of Gram-positive and Gram-negative bacteria, including beta-lactam-resistant strains.
我们之前曾报道过，通过酯键、氨基甲酸酯官能团或通过季铵氮连接喹诺酮与头孢菌素3'-位可产生具有双重抗菌作用模式的头孢菌素。我们现在描述一类新型的双重作用头孢菌素，其化学稳定性高于先前报道的那些，其中环丙沙星的碱性氮直接与3'-头孢菌素位键合，即这两个部分通过叔胺官能团相连。这些化合物已显示出对多种革兰氏阳性和革兰氏阴性细菌具有强效活性，包括β-内酰胺耐药菌株。
