Weidner Thomas, Nasereddin Abed, Preu Lutz, Grünefeld Johann, Dzikowski Ron, Kunick Conrad
Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstraße 55, 38106 Braunschweig, Germany.
Department of Microbiology and Molecular Genetics, IMRIC, The Kuvin Center for the Study of Infectious and Tropical Diseases, The Hebrew University-Hadassah Medical School, Jerusalem 91120, Israel.
Molecules. 2016 Feb 17;21(2):223. doi: 10.3390/molecules21020223.
The Tres Cantos Antimalarial Compound Set (TCAMS) is a publicly available compound library which contains 13533 hit structures with confirmed activity against Plasmodium falciparum, the infective agent responsible for malaria tropica. The TCAMS provides a variety of starting points for the investigation of new antiplasmodial drug leads. One of the promising compounds is TCMDC-137332, which seemed to be a good starting point due to its antiplasmodial potency and its predicted physicochemical properties. Several new analogues based on a 2-phenoxyanilide scaffold were synthesized by standard amide coupling reactions and were fully characterized regarding their identity and purity by spectroscopic and chromatographic methods. Furthermore, the results of the biological evaluation of all congeners against Plasmodium falciparum NF54 strains are presented. The findings of our in vitro screening could not confirm the presumed nanomolar antiplasmodial activity of TCMDC-137332 and its derivatives.
特雷斯坎托斯抗疟化合物集（TCAMS）是一个公开可用的化合物库，其中包含13533个对恶性疟原虫（导致热带疟疾的感染因子）具有确定活性的命中结构。TCAMS为新型抗疟药物先导物的研究提供了多种起点。其中一个有前景的化合物是TCMDC-137332，由于其抗疟效力和预测的物理化学性质，它似乎是一个很好的起点。通过标准酰胺偶联反应合成了几种基于2-苯氧基苯胺支架的新类似物，并通过光谱和色谱方法对其身份和纯度进行了全面表征。此外，还展示了所有同系物针对恶性疟原虫NF54菌株的生物学评价结果。我们体外筛选的结果未能证实TCMDC-137332及其衍生物假定的纳摩尔抗疟活性。
