TY - JOUR
T1 - Synthesis and biological evaluation of 2-arylbenzimidazoles targeting Leishmania donovani
AU - Keurulainen, Leena
AU - Siiskonen, Antti
AU - Nasereddin, Abedelmajeed
AU - Kopelyanskiy, Dmitry
AU - Sacerdoti-Sierra, Nina
AU - Leino, Teppo O.
AU - Tammela, Päivi
AU - Yli-Kauhaluoma, Jari
AU - Jaffe, Charles L.
AU - Kiuru, Paula
N1 - Publisher Copyright:
© 2015 Elsevier Ltd. All rights reserved.
PY - 2015/5/1
Y1 - 2015/5/1
N2 - 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.
AB - 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.
KW - 2-Arylbenzimidazoles
KW - Antileishmanial activity
KW - Biological activity
KW - Leishmania donovani
KW - Medicinal chemistry
UR - http://www.scopus.com/inward/record.url?scp=84937762490&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2015.03.027
DO - 10.1016/j.bmcl.2015.03.027
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C2 - 25827525
AN - SCOPUS:84937762490
SN - 0960-894X
VL - 25
SP - 1933
EP - 1937
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 9
ER -