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
TY - JOUR
AU - Opsenica, Igor
AU - Opsenica, Dejan
AU - Lanteri, C.A.
AU - Anova, L.
AU - Milhous, Wilbur K.
AU - Smith, K. S.
AU - Šolaja, Bogdan
PY - 2008
UR - https://cer.ihtm.bg.ac.rs/handle/123456789/448
AB - 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.
PB - American Chemical Society (ACS)
T2 - Journal of Medicinal Chemistry
T1 - New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton
VL - 51
IS - 19
SP - 6216
EP - 6219
DO - 10.1021/jm8006905
ER -
@article{
author = "Opsenica, Igor and Opsenica, Dejan and Lanteri, C.A. and Anova, L. and Milhous, Wilbur K. and Smith, K. S. and Šolaja, Bogdan",
year = "2008",
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.",
publisher = "American Chemical Society (ACS)",
journal = "Journal of Medicinal Chemistry",
title = "New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton",
volume = "51",
number = "19",
pages = "6216-6219",
doi = "10.1021/jm8006905"
}
Opsenica, I., Opsenica, D., Lanteri, C.A., Anova, L., Milhous, W. K., Smith, K. S.,& Šolaja, B.. (2008). New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton. in Journal of Medicinal Chemistry
American Chemical Society (ACS)., 51(19), 6216-6219.
https://doi.org/10.1021/jm8006905
Opsenica I, Opsenica D, Lanteri C, Anova L, Milhous WK, Smith KS, Šolaja B. New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton. in Journal of Medicinal Chemistry. 2008;51(19):6216-6219.
doi:10.1021/jm8006905 .
Opsenica, Igor, Opsenica, Dejan, Lanteri, C.A., Anova, L., Milhous, Wilbur K., Smith, K. S., Šolaja, Bogdan, "New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton" in Journal of Medicinal Chemistry, 51, no. 19 (2008):6216-6219,
https://doi.org/10.1021/jm8006905 . .
