Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners

Malaria is a severe and life-threatening disease caused by parasites that are spread to humans through bites of infected mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting parasite growth. Synthesized compounds were evaluated fo...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2017-02, Vol.22 (3), p.343
Main Authors: Konstantinović, Jelena, Videnović, Milica, Srbljanović, Jelena, Djurković-Djaković, Olgica, Bogojević, Katarina, Sciotti, Richard, Šolaja, Bogdan
Format: Article
Language:English
Subjects:
aminoquinoline
Aminoquinolines
Aminoquinolines - chemical synthesis
Aminoquinolines - chemistry
Aminoquinolines - pharmacology
Animals
Antimalarial activity
Antimalarial agents
antimalarials
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Benzothiophene
Bites
Chloroquine
Disease Models, Animal
Drug Resistance, Multiple - drug effects
Hemoglobin
Humans
Hypersensitivity
In vitro methods and tests
Kinases
Malaria
Malaria - drug therapy
Mice
Molecular Structure
Mosquitoes
Multidrug resistance
Parasites
Phosphatase
Plasmodium berghei - drug effects
Plasmodium falciparum - drug effects
Proteins
thiophene
Thiophenes - chemistry
Toxicity
Vector-borne diseases
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Summary:Malaria is a severe and life-threatening disease caused by parasites that are spread to humans through bites of infected mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC = 6 nM, and cured 5/5 infected mice when dosed orally at 160 mg/kg/day × 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules22030343