Cephalosporin 3'-quinolone esters with a dual mode of action

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Abstract
According to the generally accepted mechanism by which bacterial enzymes react with cephalosporins, opening of the .beta.-lactam ring can lead to the expulsion of a 3''-substituent. A series of dual-action cephalosporins was prepared in which antibacterial quinolones were linked to the cephalosporin 3''-position through an ester bond in the expectation that, in addition to exerting their own .beta.-lactam activity, these cephalosporins would act as prodrugs for the second antibacterial agent. Compared to parent cephalosporins in which the 3''-substituent was acetoxy, the bifunctional cephalosporins exhibited a broadened antibacterial spectrum, suggesting that a dual mode of action may indeed be operative.