Ha. Albrecht et al., DUAL-ACTION CEPHALOSPORINS INCORPORATING A 3'-TERTIARY-AMINE-LINKED QUINOLONE, Journal of medicinal chemistry, 37(3), 1994, pp. 400-407
We have previously reported that linking quinolones to the cephalospor
in 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 c
ephalosporins, with greater chemical stability than those previously r
eported, in which the basic nitrogen of ciprofloxacin is bonded direct
ly 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-neg
ative bacteria, including P-lactam-resistant strains.