Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents |
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| Authors: | Mayence Annie Vanden Eynde Jean Jacques Kaiser Marcel Brun Reto Yarlett Nigel Huang Tien L |
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| Affiliation: | aXavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel drive, New Orleans, LA 70125, USA;bUniversity of Mons-UMONS, laboratory of Organic Chemistry, 20 Place du Parc, B-7000 Mons, Belgium;cParasite Chemotherapy, Swiss Tropical Institute, Basel CH-4002, Switzerland;dUniversity of Basel, Petersplatz 1, CH-4051 Basel, Switzerland;ePace University, Department of Chemistry and Physical Sciences, and Haskins Laboratories, 1 Pace Plaza, New York, NY 10038, USA |
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| Abstract: | A small library of 26 2,2′-[alkane-α,ω-diylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and evaluated against Giardia intestinalis, Entamoeba histolytica, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum. Among the tested compounds, eight derivatives (17, 19, 20, 24, 27, 30, 32 and 35) exhibited an anti-Plasmodium falciparum activity characterized by IC50 values in the range of 180–410 nM (0.11–0.21 μg/mL) and selectivity indexes (IC50 rat skeletal myoblasts L6 cells vs IC50P. falciparum K1 strain) varying between 92 and more than 450. Two of the eight novel drug leads, namely compounds 19 and 32, were also active against G. intestinalis and L. donovani with selectivity indexes of 122 and >164 respectively. |
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| Keywords: | Benzimidazole Malaria Plasmodium Protozoan parasites |
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