Bioorganic & medicinal chemistry letters

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

BS Samant, MG Sukhthankar

Index: Samant, Bhupesh S.; Sukhthankar, Mugdha G. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 3 p. 1015 - 1018

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Citation Number: 14

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 NO2 group at the 5- ...