Antitrichomonal Agents 5-Nitrothiazoles, 5-Nitropyridines and 5-Nitropyrimidines

Abstract

Abstract Some 5-nitrothiazoles, 5-nitropyridines and 5-nitropyrimidines have been synthesised and evaluated against Trichomonas vaginalis and Trichomonas foetus in vitro and in vivo in the mouse, hamster and monkey. Although 2-amino-5-nitropyrimidine, 2-acetamido-5-nitropyrimidine and 2-trifluoroacetamido-5-nitropyrimidine were highly active in mice infected with T. vaginalis the activity was not superior to the standard 2-acetamido-5-nitrothiazole. The nitropyrimidines were highly species specific, being much more active in vivo against T. vaginalis than against T. foetus. One compound, 2-amino-5-nitropyrimidine was selected as the best of this series because of the high blood levels obtained after a single oral dose in a monkey, and its presence in a biologically active form