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New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton

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2008
Authors
Opsenica, Igor
Opsenica, Dejan
Lanteri, C.A.
Anova, L.
Milhous, Wilbur K.
Smith, K. S.
Šolaja, Bogdan
Article (Published version)
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Abstract
The synthesis of the chimeric molecules consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes 2, 4, and 8 show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, respectively. In addition, two compounds, 2 and 4, cured mice in a modified Thompson test for antimalarial blood stage activity, with a minimum curative dose of 80 mg/kg, a minimum active dose of 20 mg/kg/day, and a maximum tolerated dose of >960 mg/kg.
Source:
Journal of Medicinal Chemistry, 2008, 51, 19, 6216-6219
Publisher:
  • Amer Chemical Soc, Washington
Projects:
  • Peroksidni antimalarici i njihove himere sa hinolinima: sinteza i biološka aktivnost (RS-142022)

DOI: 10.1021/jm8006905

ISSN: 0022-2623

PubMed: 18774792

WoS: 000259760500040

Scopus: 2-s2.0-53549086186
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/448
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IHTM

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