Zhou Yuefen, Sun Zhongxiang, Froelich Jamie M, Hermann Thomas, Wall Daniel
Anadys Pharmaceuticals, Inc., San Diego, USA.
Bioorg Med Chem Lett. 2006 Oct 15;16(20):5451-6. doi: 10.1016/j.bmcl.2006.07.052. Epub 2006 Aug 4.
Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking additional aromatic moieties at the triazine C-4 position.
描述了新型细菌翻译抑制剂3,5-二氨基哌啶基三嗪系列的构效关系。优化集中在三嗪的C-4位，其中含有吸电子基团的芳族取代基可产生强效抑制剂。最初缺乏抗菌活性与细胞穿透性差有关。通过在三嗪C-4位连接额外的芳族部分实现了全细胞抗菌活性。
