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Pharmacophore model for pentamidine analogs active against Plasmodium falciparum

Athri, P. and Wenzler, T. and Tidwell, R. and Bakunova, S. M. and Wilson, W. D.. (2010) Pharmacophore model for pentamidine analogs active against Plasmodium falciparum. European Journal of Medicinal Chemistry, Vol. 45, H. 12. S. 6147-6151.

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Official URL: http://edoc.unibas.ch/dok/A5842981

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Abstract

Pentamidine and its analogs constitute a class of compounds that are known to be active against Plasmodium falciparum, which causes the most dangerous malarial infection. Malaria is a widespread disease known to affect hundreds of millions of people and presents a perceivable threat of spreading. Hence, there is a need for well-defined scaffolds that lead to new, effective treatment. Here we present a pentamidine-based pharmacophore constructed using GALAHAD that would aid targeted synthesis of leads with enhanced properties, as well as the development of lead scaffolds. The study was supported by high-quality biological in vitro data of 22 compounds against the P. falciparum strains NF54 and K1. The model established reveals the importance of hydrophobic phenyl rings with polar oxygen and amidine substituents and the hydrophobic linking chain for the activity against malaria
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:Wenzler, Tanja
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:EDIFOR
ISSN:0223-5234
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:08 Jun 2012 06:55
Deposited On:08 Jun 2012 06:46

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