Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105-3678, USA.
Bioorg Med Chem Lett. 2012 Jul 15;22(14):4536-9. doi: 10.1016/j.bmcl.2012.05.124. Epub 2012 Jun 7.
Malaria is a devastating world health problem. Using a compound library screening approach, we identified a novel series of disubstituted benzamide compounds with significant activity against malaria strains 3D7 and K1. These compounds represent a new antimalarial molecular scaffold exemplified by compound 1, which demonstrated EC(50) values of 60 and 430 nM against strains 3D7 and K1, respectively. Herein we report our findings on the efficient synthesis, structure-activity relationships, and biological activity of this new class of antimalarial agents.
疟疾是一个严重的世界性健康问题。我们采用化合物库筛选方法，发现了一系列新型的二取代苯甲酰胺化合物，对疟原虫 3D7 和 K1 株具有显著的活性。这些化合物代表了一种新的抗疟分子支架，其中化合物 1 表现出对 3D7 和 K1 株的 EC（50）值分别为 60 和 430 nM。本文报告了这种新型抗疟药物的高效合成、构效关系和生物活性的研究结果。
