Synthesis and antibacterial activity of 1beta-methyl-2-[5-(N-substituted-2-hydroxy iminoethyl)pyrrolidin-3-ylthio]carbapenem derivatives

Eur J Med Chem. 2003 Jul-Aug;38(7-8):751-8. doi: 10.1016/s0223-5234(03)00116-8.

Abstract

The synthesis of a new series of 1-methylcarbapenems having the substituted thiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. In particular, compounds 12b and 12k showed the most potent antibacterial activity.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology*
  • Carbapenems / chemical synthesis*
  • Carbapenems / pharmacology*
  • Drug Stability
  • Gram-Negative Bacteria / drug effects
  • Gram-Negative Bacteria / growth & development
  • Gram-Positive Bacteria / drug effects
  • Gram-Positive Bacteria / growth & development
  • Microbial Sensitivity Tests
  • Pseudomonas aeruginosa / drug effects
  • Pseudomonas aeruginosa / growth & development
  • Pyrrolidines / chemistry
  • Structure-Activity Relationship
  • Swine

Substances

  • Anti-Bacterial Agents
  • Carbapenems
  • Pyrrolidines