Synthesis, biological evaluation and structure-activity relationships of new quinoxaline derivatives as anti-Plasmodium falciparum agents

We report the synthesis and antimalarial activities of eighteen quinoxaline and quinoxaline 1,4-di-N-oxide derivatives, eight of which are completely novel. Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity relationships demonstrated the importance of...

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Bibliographic Details
Authors: Gil, Ana Gloria, Pabón, Adriana, Galiano, Silvia, Burguete, M. Isabel, Pérez-Silanes, Silvia, Deharo, Eric, Monge, Antonio, Aldana Ignacio
Format: article
Status:Published version
Publication Date:2014
Country:España
Institution:Consejo Superior de Investigaciones Científicas (CSIC)
Repository:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/131002
Online Access:http://hdl.handle.net/10261/131002
Access Level:Open access
Keyword:Plasmodium falciparum
Chalcone
quinoxaline 1,4-di-N-oxide
quinoxaline
Antimalarial agents
Description
Summary:We report the synthesis and antimalarial activities of eighteen quinoxaline and quinoxaline 1,4-di-N-oxide derivatives, eight of which are completely novel. Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity relationships demonstrated the importance of an enone moiety linked to the quinoxaline ring. © 2014 by the authors; licensee MDPI, Basel, Switzerland.

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