Synthesis and structure-activity relationships of 7-(2-aminoalkyl)morpholinoquinolones as anti-Helicobacter pylori agents

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2185-90. doi: 10.1016/s0960-894x(98)00390-4.

Abstract

A series of the titled compounds was synthesized and tested for anti-Helicobacter pylori activities. We discovered Y-34867 having the most potent activity against Helicobacter pylori among the quinolones tested along with high photostability. Furthermore, Y-34867 showed an excellent therapeutic effect in the experimental Helicobacter pylori infected Mongolian gerbil model.

MeSH terms

  • 4-Quinolones*
  • Animals
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Drug Stability
  • Fluoroquinolones*
  • Gerbillinae
  • Helicobacter Infections / drug therapy*
  • Helicobacter pylori / drug effects*
  • Indicators and Reagents
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Naphthyridines / pharmacology
  • Ofloxacin / pharmacology
  • Quinolones / chemical synthesis*
  • Quinolones / chemistry*
  • Quinolones / pharmacology
  • Quinolones / therapeutic use
  • Solutions
  • Structure-Activity Relationship
  • Ultraviolet Rays

Substances

  • 4-Quinolones
  • Anti-Infective Agents
  • Fluoroquinolones
  • Indicators and Reagents
  • Naphthyridines
  • Quinolones
  • Solutions
  • Y 26611
  • Ofloxacin
  • tosufloxacin
  • sparfloxacin