Novel diamidines with activity against Babesia divergens in vitro and Babesia microti in vivo.

Abstract

Dicationic diamidines, such as diminazene and pentamidine, are well-studied chemotherapeutic agents with significant activity against parasitic diseases. The in vitro activities of novel diamidine compounds against the Babesia divergens strains 1903B and 4201 were investigated. The most potent compound, a diphenyl furan, had a 50% inhibitory concentration (IC(50)) of 1.5 ng/ml. In a murine model, several test compounds were effective enough to cure mice infected with Babesia microti at a dose of 12.5 and/or 25 mg/kg of body weight given by the subcutaneous route for 4 days. The best antibabesial properties were exhibited by terphenyls, benzimidazoles, diphenyl furans, pentamidine, and pentamidine analogues.

• Authors: Angela Nehrbass-Stuedli, David Boykin, Richard R Tidwell, Reto Brun
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 55 Issue 7 Pg. 3439-45 (Jul 2011) ISSN: 1098-6596 [Electronic] United States
• PMID: 21537025 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antiprotozoal Agents
• Benzimidazoles
• Furans
• Terphenyl Compounds
• Pentamidine

Topics

• Animals
• Antiprotozoal Agents (therapeutic use)
• Babesia (drug effects, pathogenicity)
• Babesia microti (drug effects, pathogenicity)
• Babesiosis (drug therapy, parasitology)
• Benzimidazoles (therapeutic use)
• Female
• Furans (therapeutic use)
• Mice
• Parasitemia (drug therapy, parasitology)
• Pentamidine (therapeutic use)
• Terphenyl Compounds (therapeutic use)