Serveur d'exploration Chloroquine

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Synthesis and Evaluation of Antimalarial Activity of Oxygenated 3‐alkylpyridine Marine Alkaloid Analogues

Identifieur interne : 001503 ( Main/Exploration ); précédent : 001502; suivant : 001504

Synthesis and Evaluation of Antimalarial Activity of Oxygenated 3‐alkylpyridine Marine Alkaloid Analogues

Auteurs : Flaviane F. Hilário [Brésil] ; Renata Cristina De Paula [Brésil] ; Mariana L. T. Silveira [Brésil] ; Gustavo H. R. Viana [Brésil] ; Rosemeire B. Alves [Brésil] ; Juliana R. C. S. Pereira [Brésil] ; Luciana Maria Silva [Brésil] ; Rossimiriam P. De Freitas [Brésil] ; Fernando De Pilla Varotti [Brésil]

Source :

RBID : ISTEX:DB94B05280BCFCAEB5E67A01F6606C68739649E1

English descriptors

Abstract

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.
A series of new oxygenated analogues of marine 3‐alkylpyridine alkaloids were prepared from 3‐pyridinepropanol in few steps and in good yields. All new compounds were evaluated for their antiplasmodial activity and cytotoxicity. A significant reduction in parasitemia was observed for some of the prepared compounds and the majority of them exibited 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.

Url:
DOI: 10.1111/j.1747-0285.2011.01154.x


Affiliations:


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Le document en format XML

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<div type="abstract" xml:lang="en">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.</div>
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