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Identification of 1,3-diiminoisoindoline carbohydrazides as potential antimalarial candidates

Mombelli, P. and Witschel, M. C. and van Zijl, A. W. and Geist, J. G. and Rottmann, M. and Freymond, C. and Röhl, F. and Kaiser, M. and Illarionova, V. and Fischer, M. and Siepe, I. and Schweizer, W. B. and Brun, R. and Diederich, F.. (2012) Identification of 1,3-diiminoisoindoline carbohydrazides as potential antimalarial candidates. ChemMedChem, Vol. 7, H. 1. pp. 151-158.

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Official URL: http://edoc.unibas.ch/dok/A6094216

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Abstract

A series of inhibitors of plant enzymes of the non-mevalonate pathway from herbicide research efforts at BASF were screened for antimalarial activity in a cell-based assay. A 1,3-diiminoisoindoline carbohydrazide was found to inhibit the growth of Plasmodium falciparum with an IC(50) value >100 nM. Synthesis of a variety of derivatives allowed an improvement of the initial antimalarial activity down to IC(50) =18 nM for the most potent compound, the establishment of a structure-activity relationship, and the evaluation of the cytotoxic profile of the diiminoisoindolines. Furthermore, interesting configurational and conformational aspects for this class of compounds were studied by computational and X-ray crystal structure analysis. Some of the compounds can act as tridentate ligands, forming 2:1 ligand-iron(III) complexes, which also display antimalarial activity in the nanomolar IC(50) range, paired with low cytotoxicity
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Rottmann, Matthias and Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Wiley-VCH
ISSN:1860-7179
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:19 Jul 2013 07:43
Deposited On:19 Jul 2013 07:39

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