Synthesis and antiprotozoal activity of some imidazoles derivatives

Abstract

Abstract The synthesis and in vitro antiprotozoal activity of a series of nitroimidazoles are described. A substituted phenyl group and, in many of the compounds, a N-substituent were also present: vinylogues of some of the compounds are described. Several of the nitroimidazoles exhibit very high in vitro activity against Trichomonas vaginalis and T. foetus, and good activity against Histomonas meleagridis and Entamoeba histolytica. Their antifungal action was lower than that of some of the un-nitrated imidazoles. The antiprotozoal activity of these compounds is discussed in relation to their chemical structure. 4-p-Acetamidophenyl-, 4-p-chlorophenyl- and 4-(3,4-dichlorophenyl)-1-methyl-5-nitroimidazole, and 4-p-chlorophenyl- and 4-(3,4-dichlorophenyl)-1-(2-hydroxyethyl)-5-nitroimidazole are the most active against Trichomonas.