Synthesis and anti-Helicobacter pylori activity of FR182024, a new cephem derivative

Bioorg Med Chem Lett. 1999 Nov 1;9(21):3123-6. doi: 10.1016/s0960-894x(99)00549-1.

Abstract

The synthesis and anti-Helicobacter pylori activity of a novel cephem derivative FR182024 (1) are described. FR182024 having a (5-methyl-1,3,4-thiadiazol-2-yl)-thio moiety at the 3-position and a phenylacetamido at the 7-position was found to have extremely potent in vitro anti-H.pylori activity, superior therapeutic efficacy to AMPC and CAM, and low potential for causing diarrhea.

MeSH terms

  • Amoxicillin / pharmacology
  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Carbapenems / chemical synthesis*
  • Carbapenems / pharmacology
  • Clarithromycin / pharmacology
  • Disease Models, Animal
  • Helicobacter pylori / drug effects*
  • Lactams*
  • Mice
  • Molecular Structure
  • beta-Lactamases / metabolism
  • beta-Lactams / chemical synthesis*
  • beta-Lactams / pharmacology

Substances

  • Anti-Bacterial Agents
  • Carbapenems
  • Lactams
  • beta-Lactams
  • Amoxicillin
  • FR 182024
  • beta-Lactamases
  • Clarithromycin