Discovery of a novel benzyloxyisoquinoline derivative with potent anti-Helicobacter pylori activity

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1897-902. doi: 10.1016/s0960-894x(98)00335-7.

Abstract

The synthesis and in vitro optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives discovered by a random screening process, are described. FR180102 (7f), having a 3-acetamido-2,6-dichlorobenzyl moiety, was found to have extremely potent activity against H. pylori and no effect against a series of common Gram-positive and Gram-negative bacteria.

MeSH terms

  • Acetamides / chemical synthesis
  • Acetamides / chemistry
  • Acetamides / pharmacology*
  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Helicobacter pylori / drug effects*
  • Isoquinolines / chemical synthesis
  • Isoquinolines / chemistry
  • Isoquinolines / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Mice
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship

Substances

  • Acetamides
  • Anti-Bacterial Agents
  • FR 180102
  • Isoquinolines