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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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, 6216-6219Publisher:
- American Chemical Society (ACS)
Funding / projects:
DOI: 10.1021/jm8006905
ISSN: 0022-2623
PubMed: 18774792
WoS: 000259760500040
Scopus: 2-s2.0-53549086186
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IHTMTY - 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 . .