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Dual-action cephalosporins incorporating a 3'-tertiary-amine-linked quinolone
H A Albrecht1, G Beskid, J G Christenson
1Roche Research Center, Hoffmann-La Roche Incorporated, Nutley, New Jersey 07110.
Abstract:
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.