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

doi:https://doi.org/10.1016/j.bmcl.2015.03.027

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

The Hebrew University of Jerusalem

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	1933-1937
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2015.03.027
State	Published - 1 May 2015

Keywords

2-Arylbenzimidazoles
Antileishmanial activity
Biological activity
Leishmania donovani
Medicinal chemistry

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

https://doi.org/10.1016/j.bmcl.2015.03.027

Cite this

@article{6d428dbcc91b4208ae0edbb7ebdd761e,

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.",

keywords = "2-Arylbenzimidazoles, Antileishmanial activity, Biological activity, Leishmania donovani, Medicinal chemistry",

author = "Leena Keurulainen and Antti Siiskonen and Abedelmajeed Nasereddin and Dmitry Kopelyanskiy and Nina Sacerdoti-Sierra and Leino, {Teppo O.} and P{\"a}ivi Tammela and Jari Yli-Kauhaluoma and Jaffe, {Charles L.} and Paula Kiuru",

year = "2015",

month = may,

day = "1",

doi = "https://doi.org/10.1016/j.bmcl.2015.03.027",

language = "الإنجليزيّة",

volume = "25",

pages = "1933--1937",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "9",

}

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

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 - https://doi.org/10.1016/j.bmcl.2015.03.027

DO - https://doi.org/10.1016/j.bmcl.2015.03.027

M3 - مقالة

C2 - 25827525

SN - 0960-894X

VL - 25

SP - 1933

EP - 1937

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

Synthesis and biological evaluation of 2-arylbenzimidazoles targeting Leishmania donovani

Abstract

Keywords

All Science Journal Classification (ASJC) codes

Access to Document

Other files and links

Fingerprint

Cite this