New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton. Opsenica, I., Opsenica, D., Lanteri, C. A., Anova, L., Milhous, W. K., Smith, K. S., & Šolaja, B. A. J.~Med.~Chem., 51(19):6216--6219, 2008. ![New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton [link]](https://bibbase.org/img/filetypes/link.svg "link")
Paper abstract bibtex 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.
@article{Opsenica:2008aa,
Abstract = {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.},
Author = {Opsenica, Igor and Opsenica, Dejan and Lanteri, Charlotte Anne and Anova, Lalaine and Milhous, Wilbur K. and Smith, Kirsten S. and S\&{\#}x30c;olaja, Bogdan A.},
Date-Added = {2008-09-29 14:14:01 -0400},
Date-Modified = {2009-04-06 22:32:49 -0400},
Journal = {J.~Med.~Chem.},
Keywords = {malaria; artemisinin; radical; heme; epoxide},
Number = {19},
Pages = {6216--6219},
Title = {New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton},
Url = {http://pubs3.acs.org/acs/journals/doilookup?in_doi=10.1021/jm8006905},
Volume = {51},
Year = {2008},
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