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Cephalosporin derivatives (I) substituted with a neutral, acidic or basic amino acid group as the terminal group attached to the 2-amino-2-(2-aminothiazol-4-yl)acetamido side chain at the C-7 position were synthesized, and the effect of each group on antibacterial activity was examined. The derivatives bearing an amidino or guanidino group showed broad spectra of antibacterial activity similar to those of cefotaxime, but they were relatively sensitive to beta-lactamases.

journal of antibiotics

Semisynthetic .BETA.-lactam antibiotics. II Synthesis and antibacterial activity of 7.BETA.-(2-(acylamino)-2-(2-aminothiazol-4-yl)acetamido)cephalosporins.