Activity of diimidazoline amides against African trypanosomiasis

Bioorg Med Chem Lett. 2014 Feb 1;24(3):944-8. doi: 10.1016/j.bmcl.2013.12.064.

Yuxiang Dong ¹, Xiaofang Wang ¹, Monica Cal ², Marcel Kaiser ², Jonathan L Vennerstrom ³

Affiliations

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; University of Basel, CH-4003 Basel, Switzerland.
3 College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA. Electronic address: jvenners@unmc.edu.

PMID: 24398295 DOI: 10.1016/j.bmcl.2013.12.064

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

African trypanosomiasis; Diimidazoline; Trypanosoma brucei rhodesiense.

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