CER - Central Repository
Institute of Chemistry, Technology and Metallurgy
    • English
    • Српски
    • Српски (Serbia)
  • English 
    • English
    • Serbian (Cyrillic)
    • Serbian (Latin)
  • Login
View Item 
  •   CER
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
  •   CER
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

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

Authorized Users Only
2008
Authors
Opsenica, Igor
Opsenica, Dejan
Lanteri, C.A.
Anova, L.
Milhous, Wilbur K.
Smith, K. S.
Šolaja, Bogdan
Article (Published version)
Metadata
Show full item record
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:
  • American Chemical Society (ACS)
Funding / 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
[ Google Scholar ]
64
59
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/448
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
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 . .

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

re3dataOpenAIRERCUB
 

 

All of DSpaceInstitutions/communitiesAuthorsTitlesSubjectsThis institutionAuthorsTitlesSubjects

Statistics

View Usage Statistics

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

re3dataOpenAIRERCUB