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Discovery and optimisation studies of antimalarial phenotypic hits

Mital, Alka and Murugesan, Dinakaran and Kaiser, Marcel and Yeates, Clive and Gilbert, Ian H.. (2015) Discovery and optimisation studies of antimalarial phenotypic hits. European journal of medicinal chemistry, 103. pp. 530-538.

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Official URL: http://edoc.unibas.ch/41501/

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Abstract

There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falciparum K1 had EC50 values in the range of 0.09-29 μM, and generally good selectivity (typically >100-fold) compared to a mammalian cell line (L6). One example showed no significant activity against a rodent model of malaria, and more work is needed to optimise these compounds.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
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
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0223-5234
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:05 Dec 2017 10:49
Deposited On:13 Apr 2016 12:10

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