DUAL-ACTION CEPHALOSPORINS INCORPORATING A 3'-TERTIARY-AMINE-LINKED QUINOLONE

Citation
Ha. Albrecht et al., DUAL-ACTION CEPHALOSPORINS INCORPORATING A 3'-TERTIARY-AMINE-LINKED QUINOLONE, Journal of medicinal chemistry, 37(3), 1994, pp. 400-407
Citations number
29
Categorie Soggetti
Chemistry Medicinal
ISSN journal
00222623
Volume
37
Issue
3
Year of publication
1994
Pages
400 - 407
Database
ISI
SICI code
0022-2623(1994)37:3<400:DCIA3Q>2.0.ZU;2-8
Abstract
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.