3-呋喃基和3-噻吩基喹喔啉-2-甲腈1,4-二氧化物衍生物的合成及其抗疟活性
Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.
作者信息
Vicente Esther, Charnaud Sarah, Bongard Emily, Villar Raquel, Burguete Asunción, Solano Beatriz, Ancizu Saioa, Pérez-Silanes Silvia, Aldana Ignacio, Vivas Livia, Monge Antonio
机构信息
Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, 31080 Pamplona, Spain.
出版信息
Molecules. 2008 Jan 17;13(1):69-77. doi: 10.3390/molecules13010069.
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 IC(50) less than 1 microM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0.63 microM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
本研究的目的是基于我们之前对3-苯基喹喔啉-2-甲腈1,4-二氮氧化物衍生物的研究，鉴定对恶性疟原虫有活性的新化合物。合成了12种化合物并评估其抗疟活性。其中8种对3D7株的IC(50)小于1 microM。衍生物1表现出高效力（IC(50)=0.63 microM）和良好的选择性（SI=10.35），从而成为一种新的先导化合物。
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