Issue 9, 2015
From the journal:

MedChemComm

Synthesis of carboxyimidamide-substituted benzo[c][1,2,5]oxadiazoles and their analogs, and evaluation of biological activity against Leishmania donovani†

Leena Keurulainen,a   Mikko Heiskari,a   Satu Nenonen,a   Abedelmajeed Nasereddin,b   Dmitry Kopelyanskiy,b   Teppo O. Leino,a   Jari Yli-Kauhaluoma,a   Charles L. Jaffeb  and  Paula Kiuru*a  

* Corresponding authors

a Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, University of Helsinki, Viikinkaari 5 E, P. O. Box 56, FI-00014 Helsinki, Finland
E-mail: paula.kiuru@helsinki.fi

b Department of Microbiology and Molecular Genetics, IMRIC, Hebrew University-Hadassah Medical School, P. O. Box 12272, Jerusalem 9112102, Israel

Abstract

A facile synthesis route to carboxyimidamide-substituted benzoxadiazoles and related derivatives was developed. A total of 25 derivatives were synthesized. They were evaluated for antileishmanial activity by inhibition of Leishmania donovani axenic amastigote growth using a fluorescent viability microplate assay. The most promising derivative (14) demonstrated an antileishmanial EC50 of 4.0 μM, and it also showed activity in infected macrophages (EC50 5.92 μM) without signs of cytotoxicity.

Graphical abstract: Synthesis of carboxyimidamide-substituted benzo[c][1,2,5]oxadiazoles and their analogs, and evaluation of biological activity against Leishmania donovani

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Article information

DOI
https://doi.org/10.1039/C5MD00119F
Article type
Concise Article
Submitted
26 Mar 2015
Accepted
29 Jul 2015
First published
07 Aug 2015
This article is Open Access
Creative Commons BY license

Med. Chem. Commun., 2015,6, 1673-1678

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Synthesis of carboxyimidamide-substituted benzo[c][1,2,5]oxadiazoles and their analogs, and evaluation of biological activity against Leishmania donovani

L. Keurulainen, M. Heiskari, S. Nenonen, A. Nasereddin, D. Kopelyanskiy, T. O. Leino, J. Yli-Kauhaluoma, C. L. Jaffe and P. Kiuru, Med. Chem. Commun., 2015, 6, 1673 DOI: 10.1039/C5MD00119F

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