Synthesis, Biological Evaluation and Structure-Activity Relationships of New Quinoxaline Derivatives as Anti-Plasmodium falciparum Agents

Molecules

Ana Gil²  Adriana Pabón¹  Silvia Galiano²  Asunción Burguete²  Silvia Pérez-Silanes²  Eric Deharo³  Antonio Monge² 

[1] Grupo Malaria, Facultad de Medicina, Universidad de Antioquia, Medellín 050010, Colombia; E-Mail:;Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, c/ Irunlarrea 1, Pamplona 31008, Spain; E-Mails:;PHARMA-DEV, UMR 152 IRD-UPS, Faculté des Sciences Pharmaceutiques, Université Paul Sabatier, 35 chemin des Maraîchers, 31062 Toulouse Cedex 09, France; E-Mail:

关键词: Plasmodium falciparum;    antimalarial agents;    quinoxaline;    quinoxaline 1;    4-di-N-oxide;    chalcone;   

DOI  :  10.3390/molecules19022166

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.