Synthesis and evaluation of novel chloropyridazine derivatives as potent human rhinovirus (HRV) capsid-binding inhibitors

Bioorg Med Chem. 2009 Jan 15;17(2):621-4. doi: 10.1016/j.bmc.2008.11.061. Epub 2008 Dec 3.

Abstract

Human rhinovirus (HRV) is the most important etiologic agent causing common colds. No effective anti-HRV agents are currently available. In this paper we describe the synthesis and the evaluation of novel chloropyridazine derivatives (compounds 5a-g) as potent human rhinovirus (HRV) capsid-binding inhibitors. Results showed that compound 5e and 5f exhibited effective anti-HRV activity against HRV-2 and HRV-14. In addition, compound 5e and 5f showed lower cytotoxicity than Pirodavir.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Capsid Proteins / antagonists & inhibitors*
  • Common Cold / drug therapy
  • Humans
  • Pyridazines / chemical synthesis*
  • Pyridazines / pharmacology
  • Rhinovirus / drug effects*
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Capsid Proteins
  • Pyridazines
  • pyridazine