title: Synthesis and biological evaluation of 2-arylbenzimidazoles targeting Leishmania donovani.
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.
authors.affiliation: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, University of Helsinki, Viikinkaari 5 E, PO Box 56, FI-00014 Helsinki, Finland.
authors.forename: Leena
authors.initials: L
authors.lastname: Keurulainen
authors.affiliation: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, University of Helsinki, Viikinkaari 5 E, PO Box 56, FI-00014 Helsinki, Finland.
authors.forename: Antti
authors.initials: A
authors.lastname: Siiskonen
authors.affiliation: Department of Microbiology and Molecular Genetics, IMRIC, Hebrew University-Hadassah Medical School, PO Box 12272, Jerusalem 9112102, Israel.
authors.forename: Abedelmajeed
authors.initials: A
authors.lastname: Nasereddin
authors.affiliation: Department of Microbiology and Molecular Genetics, IMRIC, Hebrew University-Hadassah Medical School, PO Box 12272, Jerusalem 9112102, Israel.
authors.forename: Dmitry
authors.initials: D
authors.lastname: Kopelyanskiy
authors.affiliation: Department of Microbiology and Molecular Genetics, IMRIC, Hebrew University-Hadassah Medical School, PO Box 12272, Jerusalem 9112102, Israel.
authors.forename: Nina
authors.initials: N
authors.lastname: Sacerdoti-Sierra
authors.affiliation: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, University of Helsinki, Viikinkaari 5 E, PO Box 56, FI-00014 Helsinki, Finland.
authors.forename: Teppo O
authors.initials: TO
authors.lastname: Leino
authors.affiliation: Faculty of Pharmacy, Division of Pharmaceutical Biosciences, Centre for Drug Research, University of Helsinki, Viikinkaari 5 E, PO Box 56, FI-00014 Helsinki, Finland.
authors.forename: Päivi
authors.initials: P
authors.lastname: Tammela
authors.affiliation: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, University of Helsinki, Viikinkaari 5 E, PO Box 56, FI-00014 Helsinki, Finland.
authors.forename: Jari
authors.initials: J
authors.lastname: Yli-Kauhaluoma
authors.affiliation: Department of Microbiology and Molecular Genetics, IMRIC, Hebrew University-Hadassah Medical School, PO Box 12272, Jerusalem 9112102, Israel. Electronic address: cjaffe@cc.huji.ac.il.
authors.forename: Charles L
authors.initials: CL
authors.lastname: Jaffe
authors.affiliation: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, University of Helsinki, Viikinkaari 5 E, PO Box 56, FI-00014 Helsinki, Finland. Electronic address: paula.kiuru@helsinki.fi.
authors.forename: Paula
authors.initials: P
authors.lastname: Kiuru
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D007893:Leishmania donovani / Q000187:drug effects*; D051379:Mice; D015394:Molecular Structure; D041681:NIH 3T3 Cells; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D001562:Benzimidazoles
keywords: 2-Arylbenzimidazoles; Antileishmanial activity; Biological activity; Leishmania donovani; Medicinal chemistry