Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.
Bioorg Med Chem Lett
; 19(7): 2038-43, 2009 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-19251414
ABSTRACT
A novel series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Peróxidos
/
Plasmodium falciparum
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Quinolinas
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Antimaláricos
Limite:
Animals
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article