STRUCTURE-ACTIVITY-RELATIONSHIPS WITHIN A SERIES OF C(7)-SUBSTITUTED-OXYIMINOCEPHALOSPORINS CONTAINING THE C(3)-METHYLAMINOPYRIDINIUMTHIOMETHYL SUBSTITUENT - SYNTHESIS AND BIOLOGICAL PROPERTIES OF BRL-57342 AND SOME CLOSE ANALOGS
(6R,7R)-7-[2-(2-Amino-4-thiazolyl)-2-[(Z)-[(S)-carboxy(3,4-dihydroxyphenyl)methyl]oxyimino]acetamido]-3-(1-methylaminopyridinium- 4-thiomethyl)ceph-3-em-4-carboxylate sodium salt (BRL 57342, 1f) combines excellent in vitro antibacterial potency against Gram-positive and Gram-negative bacteria, including P. aeruginosa and Acinetobacter spp., with excellent stability to extended spectrum beta-lactamases. This potency is reflected in in vivo efficacy studies.