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Bioorganic & Medicinal Chemistry
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Bioorganic & Medicinal Chemistry
Article
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Bradford Scholars
Article . 2011
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Huprines as a new family of dual acting trypanocidal–antiplasmodial agents

Authors: Defaux, J.; Sala, M.; Formosa, X.; Galdeano, C.; Taylor, M.C.; Kelly, J.M.; Wright, Colin W.; +3 Authors

Huprines as a new family of dual acting trypanocidal–antiplasmodial agents

Abstract

A series of 19 huprines has been evaluated for their activity against cultured bloodstream forms of Trypanosoma brucei and Plasmodium falciparum. Moreover, cytotoxicity against rat myoblast L6 cells was assessed for selected huprines. All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC(50) values against T. brucei in the submicromolar to low micromolar range and selectivity indices for T. brucei over L6 cells of approximately 15, thus constituting interesting trypanocidal lead compounds. Two of these huprines were also found to be active against a chloroquine-resistant strain of P. falciparum, thus emerging as interesting trypanocidal-antiplasmodial dual acting compounds, but they exhibited little selectivity for P. falciparum over L6 cells.

Country
United Kingdom
Keywords

Medicine(all), Molecular Structure, Plasmodium falciparum, Trypanosoma brucei brucei, 4-Aminoquinolines, Heterocyclic Compounds, 4 or More Rings, Trypanocidal Agents, Article, Antimalarial agents, Rats, Antimalarials, Trypanocidal agents, Aminoquinolines, Animals, Huprines, Cells, Cultured

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    10
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Average
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
10
Average
Average
Average
Green
hybrid