title: Dual-action cephalosporins: cephalosporin 3'-quaternary ammonium quinolones.
abstract: When cephalosporins exert their biological activity by reacting with bacterial enzymes, opening of the beta-lactam ring can lead to expulsion of the 3'-substituent. A series of cephalosporins was prepared in which antibacterial quinolones were linked to the 3'-position through a quaternary nitrogen. Like the 3'-ester-linked dual-action cephalosporins reported earlier, these compounds demonstrated a broad spectrum of antibacterial activity derived from cephalosporin-like and quinolone-like components, suggesting a dual mode of action.
authors.affiliation: Roche Research Center, Hoffmann-La Roche Inc., Nutley, New Jersey 07110.
authors.forename: H A
authors.initials: HA
authors.lastname: Albrecht
authors.forename: G
authors.initials: G
authors.lastname: Beskid
authors.forename: J G
authors.initials: JG
authors.lastname: Christenson
authors.forename: J W
authors.initials: JW
authors.lastname: Durkin
authors.forename: V
authors.initials: V
authors.lastname: Fallat
authors.forename: N H
authors.initials: NH
authors.lastname: Georgopapadakou
authors.forename: D D
authors.initials: DD
authors.lastname: Keith
authors.forename: F M
authors.initials: FM
authors.lastname: Konzelmann
authors.forename: E R
authors.initials: ER
authors.lastname: Lipschitz
authors.forename: D H
authors.initials: DH
authors.lastname: McGarry
mesh_terms: D000818:Animals; D001424:Bacterial Infections / Q000188:drug therapy; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D051379:Mice; D008826:Microbial Sensitivity Tests; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D002511:Cephalosporins; D015363:Quinolones