Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis
Bhupesh S Samant1, Mugdha G Sukhthankar
1Division of Pharmaceutical chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown, South Africa. B.Samant@ru.ac.za
Abstract:
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-1H-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.
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