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Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites

Baliani, A. and Peal, V. and Gros, L. and Brun, R. and Kaiser, M. and Barrett, M. P. and Gilbert, I. H.. (2009) Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites. Organic & biomolecular chemistry : an international journal of synthetic, physical and biomolecular organic chemistry, Vol. 7, H. 6. S. 1154-1166.

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Official URL: http://edoc.unibas.ch/dok/A5843272

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Abstract

Human African trypanosomiasis (HAT), caused by the protozoan parasite Trypanosoma brucei spp., is a major health problem in sub-Saharan Africa. New drugs are urgently required for the disease. Selective uptake of toxic compounds into trypanosomes has been achieved by exploiting plasma membrane transporters. For example, the P2 aminopurine transporter, along with other transporters, selectively concentrates melamine and benzamidine moieties into trypanosomes. We have previously reported the use of the melamine motif to selectively target nitrofuran to the trypanosome. In this paper we report the further investigation of the structure activity relationships and the effect of the introduction of different functionalized substituents onto the melamine unit. Most of the compounds tested in vitro for their trypanocidal activity showed activities in the submicromolar range against T. b. rhodesiense
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:Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:Royal Society of Chemistry
ISSN:1477-0520
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:14 Sep 2012 07:17
Deposited On:14 Sep 2012 06:41

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