Novel C-2 substituted carbapenem derivatives. Part IV. Synthesis and biological activity of five membered heteroaromatic derivatives

J Antibiot (Tokyo). 1998 Feb;51(2):210-20. doi: 10.7164/antibiotics.51.210.

Abstract

The synthesis, antibacterial activity, and stability to human dehydropeptidase-1 (DHP-1) of a novel series of (5R,6S)-6-[(1R)-1-hydroxyethyl]-2-heterocyclylcarbapen-2-em-3-carb oxylates are described. Of the compounds investigated 1,5-disubstituted pyrazol-3-yl and 3-substituted isoxazol-5-yl derivatives have the best combination of antibacterial activity and stability to DHP-1. They are particularly active against community-acquired respiratory tract pathogens and have stabilities to DHP-1 superior to that of meropenem.

Publication types

  • Comparative Study

MeSH terms

  • Carbapenems / chemical synthesis*
  • Carbapenems / chemistry
  • Carbapenems / pharmacology*
  • Chromatography, High Pressure Liquid
  • Drug Stability
  • Humans
  • Microbial Sensitivity Tests
  • Spectrophotometry
  • Structure-Activity Relationship

Substances

  • Carbapenems