New N-substituted 7-aminocephalosporanic acid derivatives as potential agents against Streptococcus pneumoniae. Synthesis and in vitro activity

Bioorg Med Chem Lett. 1999 Apr 5;9(7):1035-40. doi: 10.1016/s0960-894x(99)00127-4.

Abstract

The synthesis and the antimicrobial properties of a new series of cephalosporinic beta-lactam antibiotics is described. The data reported in the present paper show the potential of this type of substituted cephalosporins as new anti Gram-positive antibiotic drugs. In fact, all compounds tested showed a good in vitro antibacterial activity against the most relevant Gram-positive pathogens including resistant species that currently represent unmet medical need. On the contrary, the new synthesized compounds were found to be completely devoid of any activity on Gram-negative bacteria up to a concentration of the single agent of 128 microg/ml.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Cephalosporins / chemical synthesis
  • Cephalosporins / chemistry*
  • Cephalosporins / pharmacology*
  • Microbial Sensitivity Tests
  • Staphylococcus aureus / drug effects
  • Streptococcus pneumoniae / drug effects*
  • Streptococcus pyogenes / drug effects
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Cephalosporins
  • 7-aminocephalosporanic acid