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Identification of a Novel Potent and SelectiveAnti-Trichomonas vaginalis Agent among Libraries of Bisbenzimidazoles
* 1 , 2, 3 , 2 , 4, 5
1  Université de Nantes, Cibles et médicaments des infections et du cancer, IICiMed, EA 1155, F-44000, Nantes, France
2  Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, LA, USA
3  Haute Ecole Provinciale de Hainaut Condorcet, B-7330 Saint-Ghislain, Belgium
4  Department of Chemistry and Physical Sciences, Pace University, New York, NY, USA
5  Haskins Laboratories, Pace University, New York, NY, USA


Small libraries of bisbenzimidazoles structurally related to pentamidine have been synthesized and evaluated against different species of parasites. 2,2’-[1,3-Propanediylbis(oxy-1,3-phenylene)]bis-1H-benzimidazole emerged as a potent and selective anti-Trichomonas vaginalis agent from in vitro and in vivo studies. In particular, in vitro under aerobic conditions the compound was more active than metronidazole against both metronidazole-susceptible (C1) and –refractory (085) isolates of Trichomonas vaginalis. In vivo, it cured a subcutaneous mouse model infection using both kinds of isolates.

Keywords: bisbenzimidazole; metronidazole; Trichomonas vaginalis