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1,2-Diphenoxiethane salts as potent antiplasmodial agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-05-31 , DOI: 10.1016/j.bmcl.2018.05.060 Santiago Schiafino-Ortega , Eleonora Baglioni , Guiomar Pérez-Moreno , Pablo Rios Marco , Carmen Marco , Dolores González-Pacanowska , Luis Miguel Ruiz-Pérez , María Paz Carrasco-Jiménez , Luisa Carlota López-Cara
中文翻译:
1,2-二苯氧乙烷盐类作为有效的抗疟原虫药
更新日期:2018-05-31
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-05-31 , DOI: 10.1016/j.bmcl.2018.05.060 Santiago Schiafino-Ortega , Eleonora Baglioni , Guiomar Pérez-Moreno , Pablo Rios Marco , Carmen Marco , Dolores González-Pacanowska , Luis Miguel Ruiz-Pérez , María Paz Carrasco-Jiménez , Luisa Carlota López-Cara
In this article we present a series of non-cytotoxic potent human choline kinase (CK) inhibitors that exhibit nanomolar antiplasmodial activity in vitro. The most active antiplasmodial compounds, 10a–b, bearing a pyridinium cationic head were inactive against CK, while compounds 10g and 10j with a quinolinium moiety exhibit moderate inhibition of both the parasite and the enzyme. The results point towards an additional mechanism of action unrelated to CK inhibition that remains to be established.
中文翻译:
1,2-二苯氧乙烷盐类作为有效的抗疟原虫药
在本文中,我们介绍了一系列在体外表现出纳摩尔抗血浆活性的非细胞毒性有效人胆碱激酶(CK)抑制剂。带有吡啶鎓阳离子头的活性最高的抗疟原虫化合物10a – b对CK无活性,而具有喹啉部分的化合物10g和10j对寄生虫和酶均具有中等抑制作用。结果指向与CK抑制无关的另外的作用机制,尚待建立。