Synthesis and antiparasitic activity of 1H-benzimidazole derivatives

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2221-4. doi: 10.1016/s0960-894x(02)00346-3.

Abstract

Compounds 1-18 have been synthesized and tested in vitro against the protozoa Giardia lamblia, Entamoeba histolytica and the helminth Trichinella spiralis. Inhibition of rat brain tubulin polymerization was also measured and compared for each compound. Results indicate that most of the compounds tested were more active as antiprotozoal agents than Metronidazole and Albendazole. None of the compounds was as active as Albendazole against T. spiralis. Although only compounds 3, 9 and 15 (2-methoxycarbonylamino derivatives) inhibited tubulin polymerization, these were not the most potent antiparasitic compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Albendazole / pharmacology
  • Animals
  • Antiparasitic Agents / chemical synthesis*
  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / pharmacology*
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Brain
  • Eukaryota / drug effects
  • Metronidazole / pharmacology
  • Molecular Structure
  • Rats
  • Trichinella spiralis / drug effects
  • Tubulin / metabolism

Substances

  • Antiparasitic Agents
  • Benzimidazoles
  • Tubulin
  • Metronidazole
  • Albendazole