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  • Title: Synthesis and biological evaluation of 2-arylbenzimidazoles targeting Leishmania donovani.
    Author: Keurulainen L, Siiskonen A, Nasereddin A, Kopelyanskiy D, Sacerdoti-Sierra N, Leino TO, Tammela P, Yli-Kauhaluoma J, Jaffe CL, Kiuru P.
    Journal: Bioorg Med Chem Lett; 2015 May 01; 25(9):1933-7. PubMed ID: 25827525.
    Abstract:
    A set of 56 2-arylbenzimidazoles was designed, synthesized and tested against Leishmania donovani amastigotes. The left- and right-hand side rings of the molecule, as well as the amide linker were modified. Structurally different derivatives were screened on L. donovani axenic amastigotes at concentrations of 5, 15 and 50 μM, and the ten most active derivatives were selected for further testing. 2-Arylbenzimidazole derivative 24 was active against L. donovani-infected THP-1 cells showing 46% parasite inhibition at 5 μM.
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