Synthesis, selective anti-Helicobacter pylori activity, and cytotoxicity of novel N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4922-6. doi: 10.1016/j.bmcl.2010.06.048. Epub 2010 Jun 19.

Abstract

N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for selective antibacterial activity against 20 isolates of Helicobacter pylori clinical strains, including five metronidazole resistant ones. Some of them possessed the best activity against H. pylori metronidazole resistant strains with MIC values lower than the drug reference (metronidazole). Furthermore, anti-inflammatory activity through the inhibition of the IL-8 production was investigated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / toxicity
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / toxicity
  • Cell Line
  • Coumarins / chemical synthesis
  • Coumarins / chemistry*
  • Coumarins / toxicity
  • Drug Resistance, Bacterial
  • Helicobacter pylori / drug effects*
  • Helicobacter pylori / isolation & purification
  • Humans
  • Interleukin-8 / metabolism
  • Metronidazole / pharmacology
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Anti-Inflammatory Agents
  • Coumarins
  • Interleukin-8
  • Metronidazole
  • coumarin