Synthesis of metronidazole derivatives as antigiardiasis agents

Metronidazole (MTZ) and its derivatives have been extensively used to treat infections caused by protozoa and anaerobic bacteria. In this investigation several novel imidazole and nitroimidazol derivatives namely: 2-(1H-1-imidazolyl)-1-phenyl-1-ethanol 1a, 2-(2-methyl-1H-1-imidazolyl)-1-phenyl-1-ethanol 1b, 2-(2-methyl-4-nitro-1H-1-imidazolyl)-1-phenyl-1-ethanol 1c, 2-(1H-1-imidazolyl)-1-cyclohexanol 2d and 2-(2-methyl-4-nitro-1H-1-imidazolyl)-1-cyclohexanol 2e were prepared by the reaction of the corresponding imidazoles with styrene oxide or cyclohexene oxide respectively and their biological activity against Giardia lamblia cyst in compareison with MTZ were determined by flotation technique based on Bingham method. These compounds were less active than metronidazole but showed significant antigiardiasis activity.