Novel 1beta-methylcarbapenems with isoxazoloethenyl moieties containing carboxylic acid sodium salt

Bioorg Med Chem Lett. 2005 Jan 3;15(1):231-4. doi: 10.1016/j.bmcl.2004.09.092.

Abstract

The synthesis of novel 1beta-methylcarbapenems 1a,b having sodium 5-(3- and 5-carboxylic acid)isoxazoloethenyl moieties at C-5 position of pyrrolidine ring and their biological evaluation are described. Both compounds showed potent and well-balanced antibacterial activity as well as high stability to DHP-I. The selected sodium 3-carboxylic acid derivative 1a possessed excellent DHP-I stability and advanced pharmacokinetic parameters in comparison with 2 and meropenem.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Area Under Curve
  • Carbapenems / chemistry
  • Carbapenems / pharmacokinetics
  • Carbapenems / pharmacology*
  • Carboxylic Acids / analysis*
  • Drug Evaluation, Preclinical
  • Drug Stability
  • Microbial Sensitivity Tests

Substances

  • 1 beta-methylcarbapenem
  • Anti-Bacterial Agents
  • Carbapenems
  • Carboxylic Acids