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Synthesis and Evaluation of Antimalarial Activity of Oxygenated 3‐alkylpyridine Marine Alkaloid Analogues
Author(s) -
Hilário Flaviane F.,
de Paula Renata Cristina,
Silveira Mariana L. T.,
Viana Gustavo H. R.,
Alves Rosemeire B.,
Pereira Juliana R. C. S.,
Silva Luciana Maria,
de Freitas Rossimiriam P.,
de Pilla Varotti Fernando
Publication year - 2011
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2011.01154.x
Subject(s) - chemistry , cytotoxicity , alkaloid , plasmodium falciparum , selectivity , stereochemistry , combinatorial chemistry , antimalarial agent , organic chemistry , biochemistry , biology , in vitro , malaria , immunology , catalysis
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.