Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis

A series of compounds containing a 2-substituted imidazole ring has been synthesized from imidazole and tested for its biological activity against human African trypanosomiasis (HAT) along with its cytotoxicity and solubility. A series of compounds containing 2-substituted imidazoles has been synthesized from imidazole and tested for its biological activity against human African trypanosomiasis (HAT). The 2-substituted 5-nitroimidazoles such as fexinidazole ( 7a ) and 1-[4-(1-methyl-5-nitro-1 H -imidazol-2-ylmethoxy)-pyridin-2-yl-piperazine ( 9e ) exhibited potent activity against T. brucei in vitro with low cytotoxicity and good solubility. The presence of the NO 2 group at the 5-position of the imidazole ring in 2-substituted imidazoles is the crucial factor to inhibit T. brucei .