Synthesis and evaluation of new difluoromethyl azoles as antileishmanial agents

Eur J Med Chem. 2007 Nov-Dec;42(11-12):1388-95. doi: 10.1016/j.ejmech.2007.02.020. Epub 2007 Mar 12.

Abstract

Several compounds of great pharmacological interest contain the triazole and imidazole rings. In order to find new drugs with antileishmanial activity we have synthesized and evaluated new imidazole and triazole compounds carrying either the carbaldehyde or the difluoromethylene functionalities against promastigote forms of Leishmania amazonensis. Among the compounds tested difluoromethylene azoles 4b and 8f have inhibited the parasite growth significantly. Our results show that the introduction of the difluoromethylene moieties has turned the inactive carbaldehydes into active antileishmanial compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Azoles / chemical synthesis*
  • Azoles / chemistry
  • Azoles / pharmacology*
  • Female
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Leishmania mexicana / drug effects*
  • Triazoles / chemical synthesis
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Antiprotozoal Agents
  • Azoles
  • Imidazoles
  • Triazoles
  • imidazole