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Activity of diimidazoline amides against African trypanosomiasis
Affiliation:1. College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA;2. Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland;3. University of Basel, CH-4003 Basel, Switzerland;1. Armauer Hansen Research Institute, Addis Ababa, Ethiopia;2. Ethiopian Public Health Institute, Addis Ababa, Ethiopia;3. Amhara Regional State Referral and Research Laboratory, Bahir Dar, Ethiopia;4. University of Lübeck, Lübeck, Germany;1. College of Chemistry and Chemical Engineering, Fujian Normal University, Fuzhou 350007, PR China;2. Fujian Key Laboratory of Polymer Materials, Fuzhou 350007, PR China;1. Department of Critical Care Medicine, Hospital for Sick Children, University of Toronto, 555 University Avenue, Toronto, Ontario M5G 1X8, Canada;2. Tropical Disease Unit, Department of Medicine, Toronto General Hospital, University of Toronto, 200 Elizabeth Street, 13N-1347, Toronto, Ontario M5G 2C4, Canada;3. Department of Paediatrics and Emergency Medicine, Global Child Health, University of British Columbia, B245, 4480 Oak Street, Vancouver, British Columbia V6H 3V4, Canada
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.
Keywords:Diimidazoline  African trypanosomiasis
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