具有体外杀锥虫活性的喹喔啉二-N-氧化物衍生物的合成及生物学评价
Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity.
作者信息
Pérez-Silanes Silvia, Torres Enrique, Arbillaga Leire, Varela Javier, Cerecetto Hugo, González Mercedes, Azqueta Amaya, Moreno-Viguri Elsa
机构信息
Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain; Institute of Tropical Health, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain.
Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain.
出版信息
Bioorg Med Chem Lett. 2016 Feb 1;26(3):903-906. doi: 10.1016/j.bmcl.2015.12.070. Epub 2015 Dec 21.
We report the synthesis and in vitro activity against Trypanosoma cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 μM. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.
我们报道了15种新型喹喔啉衍生物的合成及其对克氏锥虫前鞭毛体的体外活性。其中10种衍生物的半数抑制浓度（IC50）值低于参考药物硝呋替莫（Nfx）和苄硝唑（Bzn）；其中4种衍生物表现突出，IC50值低于1.5 μM。此外，还报道了非特异性细胞毒性和遗传毒性研究。化合物14的选择性指数（SI）高于24，而化合物10是遗传毒性筛选中唯一呈阴性的化合物。
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