title: Activity of diimidazoline amides against African trypanosomiasis.
abstract: We identified several diimidazoline mono- and diamides that were as potent as pentamidine against Trypanosoma brucei rhodesiense in vitro. All of these were also less cytotoxic than pentamidine, but none was as effective as the latter in a T. brucei rhodesiense-infected mouse model. A single imidazoline may be sufficient for high antitrypanosomal activity provided that a second weak base functional group is present.
authors.affiliation: College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
authors.forename: Yuxiang
authors.initials: Y
authors.lastname: Dong
authors.affiliation: College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
authors.forename: Xiaofang
authors.initials: X
authors.lastname: Wang
authors.affiliation: Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
authors.forename: Monica
authors.initials: M
authors.lastname: Cal
authors.affiliation: Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.affiliation: College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA. Electronic address: jvenners@unmc.edu.
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Vennerstrom
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D004195:Disease Models, Animal; D006801:Humans; D048288:Imidazolines / Q000737:chemistry / Q000627:therapeutic use*; D051379:Mice; D015394:Molecular Structure; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects*; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D000577:Amides; D048288:Imidazolines; D014344:Trypanocidal Agents
keywords: African trypanosomiasis; Diimidazoline; Trypanosoma brucei rhodesiense