Structure–activity relationships of novel antibacterial translation inhibitors: 3, 5-Diamino-piperidinyl triazines

Y Zhou, Z Sun, JM Froelich, T Hermann…

Index: Zhou, Yuefen; Sun, Zhongxiang; Froelich, Jamie M.; Hermann, Thomas; Wall, Daniel Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 20 p. 5451 - 5456

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Citation Number: 40

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 ...