杂环-2-羧酸（3-氰基-1,4-二-N-氧化物喹喔啉-2-基）酰胺衍生物作为被忽视疾病药物开发的先导化合物。
Heterocyclic-2-carboxylic acid (3-cyano-1,4-di-N-oxidequinoxalin-2-yl)amide derivatives as hits for the development of neglected disease drugs.
作者信息
Ancizu Saioa, Moreno Elsa, Torres Enrique, Burguete Asunción, Pérez-Silanes Silvia, Benítez Diego, Villar Raquel, Solano Beatriz, Marín Adoración, Aldana Ignacio, Cerecetto Hugo, González Mercedes, Monge Antonio
机构信息
Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada, University of Navarra, C/Irunlarrea s/n, 31008 Pamplona, Spain.
出版信息
Molecules. 2009 Jun 22;14(6):2256-72. doi: 10.3390/molecules14062256.
Abstract
Neglected diseases represent a major health problem. It is estimated that one third of the world population is infected with tuberculosis (TB). Besides TB, Chagas disease, affects approximately 20 million people. Quinoxalines display great activities against TB and Chagas. Forty new quinoxaline 1,4-di-N-oxide derivatives have been prepared and tested against M. tuberculosis and T. cruzi. Carboxylic acid quinoxaline 1,4-di-N-oxides (CAQDOs) 5 and 17 showed MIC values on the same order as the reference antituberculosis drug, rifampicin. Meanwhile, CAQDOs 12 and 22 presented IC(50) values in the same order as the anti-chagasic drug, nifurtimox.
摘要
被忽视的疾病是一个重大的健康问题。据估计，世界三分之一的人口感染了结核病（TB）。除了结核病，恰加斯病影响着约2000万人。喹喔啉对结核病和恰加斯病显示出强大的活性。已经制备了40种新的喹喔啉1,4 - 二氮氧化物衍生物，并针对结核分枝杆菌和克氏锥虫进行了测试。羧酸喹喔啉1,4 - 二氮氧化物（CAQDOs）5和17的最低抑菌浓度（MIC）值与抗结核药物利福平处于同一水平。同时，CAQDOs 12和22的半数抑制浓度（IC50）值与抗恰加斯病药物硝呋替莫处于同一水平。
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