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Published on: May 9, 2025
Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-diamino-piperidinyl triazines
Yuefen Zhou1, Zhongxiang Sun, Jamie M Froelich
1Anadys Pharmaceuticals, Inc., San Diego, USA.
Abstract:
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.
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