Synthesis and in vitro selective anti-Helicobacter pylori activity of pyrazoline derivatives

Bioorg Med Chem Lett. 2005 Feb 1;15(3):603-7. doi: 10.1016/j.bmcl.2004.11.042.

Abstract

In order to develop new anti-Helicobacter pylori agents, a series of N1-substituted 3,5-diphenyl pyrazolines P1-P13 was prepared and evaluated for their antibacterial activity. All synthesized compounds showed little or no activity against different species of Gram-positive and Gram-negative bacteria of clinical relevance and against various strains of pathogenic fungi. The same derivatives exhibited a significant degree of activity against a range of H. pylori strains, including those resistant to the reference compound metronidazole. Among the prepared compounds those with an N1-acetyl group and a 4-methoxy substituent in the 5-phenyl ring showed the best activity against H. pylori metronidazole resistant strains in the 1-4 microg/mL MIC range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Drug Resistance
  • Helicobacter pylori / drug effects*
  • Humans
  • Metronidazole
  • Microbial Sensitivity Tests
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Species Specificity
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Pyrazoles
  • Metronidazole