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The synthesis of a series of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido]-3-(4,6-diamino-1-alkyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylates is described. Variations of an oxyimino moiety in the 7-side chain and quaternary ammonium moiety in the 3-side chain were examined and structure-activity relationship was studied. The 4,6-diamino-1-methyl-1,3,5-triazinium-2-yl derivative of the 7-α-methoxyimino series of cephalospoins, particularly 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-(4,6-diamino-1-methyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylate(C-1), exhibited broad antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.
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