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Chem Biol Drug Des ; 78(3): 477-82, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21668650

RESUMO

A series of new oxygenated analogues of marine 3-alkylpyridine alkaloids were prepared from 3-pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a Williamson etherification under phase-transfer conditions. All new compounds were evaluated for their antiplasmodial activity and cytotoxicity. A significant reduction in parasitaemia was observed for some of the prepared compounds, and the majority of them exhibited a selectivity index (SI) ranging from 2.78 to 15.58, which suggests that these compounds may be a promising class of substances with antimalarial activity.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Antimaláricos/química , Antimaláricos/farmacologia , Malária Falciparum/tratamento farmacológico , Plasmodium falciparum/efeitos dos fármacos , Alcaloides/síntese química , Antimaláricos/síntese química , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Piridinas/síntese química , Piridinas/química , Piridinas/farmacologia , Relação Estrutura-Atividade
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