Synthesis and Antiplasmodial Activity of 3-Furyl and3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives†

Molecules

Esther Vicente²  Sarah Charnaud¹  Emily Bongard¹  Raquel Villar²  Asunción Burguete²  Beatriz Solano²  Saioa Ancizu²  Silvia Pérez-Silanes²  Ignacio Aldana²  Livia Vivas¹ 

[1] Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine (LSHTM), Keppel Street, London WC1E 7HT, United Kingdom;Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, 31080 Pamplona, Spain

关键词: Quinoxaline;    N-oxides;    malaria;    antiplasmodial;    P. falciparum;   

DOI  :  10.3390/molecules13010069

来源: mdpi

【 摘 要 】

The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC₅₀ < 1 μM against the 3D7 strain. Derivative 1 demonstrated high potency (IC₅₀= 0.63 µM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.

【 授权许可】

Unknown   
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