Synthesis and antibacterial activity of 1 beta-methyl-2-(5-substituted imidazolino pyrrolidin-3-ylthio)carbapenem derivatives

Arch Pharm (Weinheim). 2003 Nov;336(11):504-9. doi: 10.1002/ardp.200300756.

Abstract

The synthesis of a new series of 1 beta-methylcarbapenems containing a substituted imidazolino pyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the imidazoline ring was investigated. Compound 13 g which has a N-sulfonylmethyl substituted imidazoline moiety showed the most potent antibacterial activity.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Carbapenems / chemical synthesis*
  • Carbapenems / chemistry
  • Carbapenems / pharmacology
  • Drug Stability
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Pyrrolidines / chemical synthesis*
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Carbapenems
  • Pyrrolidines