Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains.
Bioorg Chem
; 70: 74-85, 2017 02.
Article
em En
| MEDLINE
| ID: mdl-27908538
ABSTRACT
In the present study we have synthesized a new class of 4-aminoquinolines and evaluated against Plasmodium falciparum in vitro (3D7-sensitive strain & K1-resistant strain) and Plasmodium yoelii in vivo (N-67 strain). Among the series, eleven compounds (5, 6, 7, 8, 9, 11, 12, 13, 14, 15 and 21) showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogues showed 100% suppression of parasitemia on day 4 in the in vivo mouse model against N-67 strain when administered orally. Further, biophysical studies suggest that this series of compounds act on heme polymerization target.
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Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
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Plasmodium yoelii
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Aminoquinolinas
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Malária
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Antimaláricos
Limite:
Animals
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Humans
Idioma:
En
Revista:
Bioorg Chem
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Índia