SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NOVEL CEPHALOSPORINS CONTAINING A (Z)-VINYL DIMETHYLPHOSPHONATE GROUP

A series of cephalosporins containing a novel iazol-4-yl)-3-(dimethoxy phosphoryl)-acryloylamino] group were prepared and their antibacterial activity measured against a range of pathogens. In general the compou nds displayed a broad spectrum of activity against both Gram positive and Gram negative organisms, except Pseudomonas aeruginosa. Activity a gainst the latter could be achieved by introducing a catechol moiety a t the 3 position of the cephalosporin. The methyl phosphonates in gene ral were stable to a wide range of beta-lactamases, including the TEM enzymes and the Enterobacter cloacae P99 chromosomal enzyme. In additi on, they showed the advantage of being highly water soluble.