New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton
Само за регистроване кориснике
2008
Аутори
Opsenica, IgorOpsenica, Dejan M.
Lanteri, Charlotte Anne
Anova, Lalaine
Milhous, Wilbur K.
Smith, Kirsten S.
Šolaja, Bogdan A.
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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 gt 960 mg/kg.
Извор:
Journal of Medicinal Chemistry, 2008, 51, 19, 6216-6219Издавач:
- Amer Chemical Soc, Washington
Финансирање / пројекти:
- Пероксидни антималарици и њихове химере са хинолинима: синтеза и биолошка активност (RS-MESTD-MPN2006-2010-142022)
- U.S. National Institute of Allergy and Infectious Diseases
- Serbian Academy of Sciences and Arts.
DOI: 10.1021/jm8006905
ISSN: 0022-2623
PubMed: 18774792
WoS: 000259760500040
Scopus: 2-s2.0-53549086186
Колекције
Институција/група
Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Opsenica, Igor AU - Opsenica, Dejan M. AU - Lanteri, Charlotte Anne AU - Anova, Lalaine AU - Milhous, Wilbur K. AU - Smith, Kirsten S. AU - Šolaja, Bogdan A. PY - 2008 UR - https://cherry.chem.bg.ac.rs/handle/123456789/975 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 gt 960 mg/kg. PB - Amer Chemical Soc, Washington 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 M. and Lanteri, Charlotte Anne and Anova, Lalaine and Milhous, Wilbur K. and Smith, Kirsten S. and Šolaja, Bogdan A.", 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 gt 960 mg/kg.", publisher = "Amer Chemical Soc, Washington", 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. M., Lanteri, C. A., Anova, L., Milhous, W. K., Smith, K. S.,& Šolaja, B. A.. (2008). New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton. in Journal of Medicinal Chemistry Amer Chemical Soc, Washington., 51(19), 6216-6219. https://doi.org/10.1021/jm8006905
Opsenica I, Opsenica DM, Lanteri CA, Anova L, Milhous WK, Smith KS, Šolaja BA. 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 M., Lanteri, Charlotte Anne, Anova, Lalaine, Milhous, Wilbur K., Smith, Kirsten S., Šolaja, Bogdan A., "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 . .