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/Author (Opsenica, Igor and Selakovic, Milica and Tot, Miklos and Verbic, Tatjana and Srbljanovic, Jelena and Stajner, Tijana and Djurkovic-Djakovic, Olgica and Solaja, Bogdan)
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/Title ({New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria})
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/bibtex#2FDOI (10.2298/jsc201225005o)
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/Keywords (antimalarials,bromobenzyl derivatives,quinoline,$\\beta$-hematin inhi-bitory activity)
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/Subject (Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 \(CQ susceptible clone\) and Dd2 \(CQ resistant clone\). Three amino-quinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Anti-malarial 3 was found toxic at a dose of 320 \(mg/kg\)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured.)
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Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three amino-quinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Anti-malarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured.
Igor Opsenica
Milica Selakovic
Miklos Tot
Tatjana Verbic
Jelena Srbljanovic
Tijana Stajner
Olgica Djurkovic-Djakovic
Bogdan Solaja
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bibtex/journal/J. Serb. Chem. Soc.
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bibtex/number/02
bibtex/pages/115--123
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10.2298/jsc201225005o
antimalarials
bromobenzyl derivatives
quinoline
$\beta$-hematin inhi-bitory activity
Serbian Chemical Society
{New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria}
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