Structure-activity relationships within a series of C(7)-substitutedoxyiminocephalosporins containing the C(3)-methylaminopyridiniumthiomethyl substituent. Synthesis and biological properties of BRL 57342 and some close analogues

J Antibiot (Tokyo). 1995 May;48(5):417-24. doi: 10.7164/antibiotics.48.417.

Abstract

(6R,7R)-7-[2-(2-Amino-4-thiazolyl)-2-[(Z)-[(S)-carboxy(3,4- dihydroxyphenyl)methyl]oxyimino]acetamido]-3-(1-methylaminopyri dinium-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.

MeSH terms

  • Animals
  • Cephalosporins / chemical synthesis*
  • Cephalosporins / chemistry
  • Cephalosporins / pharmacology
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Humans
  • Mice
  • Microbial Sensitivity Tests
  • Saimiri
  • Structure-Activity Relationship

Substances

  • BRL 57342
  • Cephalosporins