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Identification of a new chemical class of antimalarials

Brunner, R. and Aissaoui, H. and Boss, C. and Bozdech, Z. and Brun, R. and Corminboeuf, O. and Delahaye, S. and Fischli, C. and Heidmann, B. and Kaiser, M. and Kamber, J. and Meyer, S. and Papastogiannidis, P. and Siegrist, R. and Voss, Till S. and Welford, R. and Wittlin, S. and Binkert, C.. (2012) Identification of a new chemical class of antimalarials. Journal of infectious diseases, Vol. 206, no. 5. pp. 735-743.

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Official URL: http://edoc.unibas.ch/dok/A6094218

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Abstract

The increasing spread of drug-resistant malaria strains underscores the need for new antimalarial agents with novel modes of action (MOAs). Here, we describe a compound representative of a new class of antimalarials. This molecule, ACT-213615, potently inhibits in vitro erythrocytic growth of all tested Plasmodium falciparum strains, irrespective of their drug resistance properties, with IC(50) values in the low single-digit nanomolar range. Like the clinically used artemisinins, the compound equally and very rapidly affects all three asexual erythrocytic parasite stages. In contrast, microarray studies suggest that the MOA of ACT-213615 is different from that of the artemisinins and other known antimalarials.ACT-213615 is orally bioavailable in mice, exhibits activity in the murine P. berghei model and efficacy comparable to that of the reference drug chloroquine in the recently established P. falciparum SCID mouse model.ACT-213615 represents a new class of potent antimalarials that merits further investigation for its clinical potential
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:Kaiser, Marcel and Wittlin, Sergio and Brun, Reto and Voss, Till S
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Oxford University Press
ISSN:0022-1899
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:06 Nov 2018 13:34
Deposited On:19 Jul 2013 07:39

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