S-3578, A new broad spectrum parenteral cephalosporin exhibiting potent activity against both methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa synthesis and structure-activity relationships

Abstract

A series of 7-aminothiadiazolylcephalosporins having a 1-(substituted)-1H-imidazo[4,5-b]pyridinium group at the C-3′ position of the cephem nucleus were synthesized and evaluated for in vitro antibacterial activities. Among the cephalosporins prepared in this study, -(3-methylaminopropyl)-1Himidazo[4,5-b]pyridinium-4-yl]methyl-3-cephem-4 -carboxylate sulfate (S-3578) showed extremely potent broad spectrum activity against both Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and Gram-negative bacteria including Pseudomonas aeruginosa, and good water solubility.