Antiprotozoal activity of proton-pump inhibitors

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7351-4. doi: 10.1016/j.bmcl.2011.10.028. Epub 2011 Oct 14.

Abstract

Parasitic diseases are still a major health problem in developing countries. In our effort to find new antiparasitic agents, in this Letter we report the in vitro antiprotozoal activity of omeprazole, lansoprazole, rabeprazole and pantoprazole against Trichomonas vaginalis, Giardia intestinalis and Entamoeba histolytica. Molecular modeling studies were an important tool to highlight the potential antiprotozoal activity of these drugs. Experimental evaluations revealed a strong activity for all compounds tested. Rabeprazole and pantoprazole were the most active compounds, having IC(50) values in the nanomolar range, which were even better than metronidazole, the drug of choice for these parasites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Pyridinylmethylsulfinylbenzimidazoles / chemistry
  • 2-Pyridinylmethylsulfinylbenzimidazoles / pharmacology
  • Antiprotozoal Agents / chemistry*
  • Antiprotozoal Agents / pharmacology
  • Drug Design
  • Entamoeba histolytica / drug effects
  • Giardia lamblia / drug effects
  • Humans
  • Lansoprazole
  • Omeprazole / chemistry
  • Omeprazole / pharmacology
  • Pantoprazole
  • Parasitic Diseases / drug therapy
  • Proton Pump Inhibitors / chemistry*
  • Proton Pump Inhibitors / pharmacology
  • Rabeprazole
  • Trichomonas vaginalis / drug effects

Substances

  • 2-Pyridinylmethylsulfinylbenzimidazoles
  • Antiprotozoal Agents
  • Proton Pump Inhibitors
  • Lansoprazole
  • Rabeprazole
  • Pantoprazole
  • Omeprazole