title: Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.
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.
authors.affiliation: Division of Pharmaceutical chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown, South Africa. B.Samant@ru.ac.za
authors.forename: Bhupesh S
authors.initials: BS
authors.lastname: Samant
authors.forename: Mugdha G
authors.initials: MG
authors.lastname: Sukhthankar
mesh_terms: D000818:Animals; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D012995:Solubility; D013237:Stereoisomerism; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy*
chemical_list: D007093:Imidazoles; D014344:Trypanocidal Agents; C029899:imidazole