Synthesis and biological evaluation of 2-arylbenzimidazoles targeting Leishmania donovani

Leena Keurulainen, Antti Siiskonen, Abedelmajeed Nasereddin, Dmitry Kopelyanskiy, Nina Sacerdoti-Sierra, Teppo O. Leino, Päivi Tammela, Jari Yli-Kauhaluoma, Charles L. Jaffe, Paula Kiuru*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

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.

Original languageAmerican English
Pages (from-to)1933-1937
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number9
DOIs
StatePublished - 1 May 2015

Bibliographical note

Publisher Copyright:
© 2015 Elsevier Ltd. All rights reserved.

Keywords

  • 2-Arylbenzimidazoles
  • Antileishmanial activity
  • Biological activity
  • Leishmania donovani
  • Medicinal chemistry

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