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Synthesis and Structure-Activity Relationship of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives against Plasmodium falciparumclick to see Communication
E. Vicente
* 1, 2 ,
R. Villar
1 ,
A. Burguete
1 ,
B. Solano
1 ,
S. Pérez-Silanes
1 ,
I. Aldana
1 ,
L. Vivas
2 ,
A. Monge
1
1  Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología, Aplicada (CIFA), University of Navarra, 31080 Pamplona, Spain.
2  Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, (LSHTM), Keppel Street, London WC1E 7HT, United Kingdom
Published: 30 November 2007 by MDPI in The 11th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic Chemistry and Natural Products
https://doi.org/10.3390/ecsoc-11-01341
Abstract: The aim of this study was to identify new active compounds against Plasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2- carbonitrile 1,4-di-N-oxide derivatives. Antimalarial activity was evaluated in vitro against Plasmodium falciparum (3D7 and K1 strains) by the incorporation of [ 3 H]hypoxanthine. Cytotoxicity was tested in KB cells by Alamar Blue assay. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed a IC 50 < 1 µM against 3D7 strain. Derivative 1 demonstrated high potency (IC 50 = 0.63 µM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
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