Triaminotriazine DNA helicase inhibitors with antibacterial activity
Triaminotriazine DNA helicase inhibitors with antibacterial activity
复制标题
DOI：
10.1016/j.bmcl.2005.11.076
复制
发表时间：
2006-03-01
影响因子：
2.7
通讯作者：
Far, AR
中科院分区：
文献类型：
--
作者：
McKay, GA;Reddy, R;Far, AR
在涉及铜绿假单胞菌DnaB解旋酶的DNA解旋酶测定中筛选化学文库提供了具有良好抗菌活性但对哺乳动物细胞具有相关细胞毒性的三氨基三嗪抑制剂。类似物的合成提供了一些抑制剂，保留抗菌活性，并表现出显着降低细胞毒性。血清的影响和对作用模式的初步研究突出了这类化合物作为抗菌剂的几个特征。(C)2005 Elsevier Ltd.保留所有权利。
Screening of a chemical library in a DNA helicase assay involving the Pseudomonas aeruginosa DnaB helicase provided a triaminotriazine inhibitor with good antibacterial activity but associated cytotoxicity toward mammalian cells. Synthesis of analogs provided a few inhibitors that retained antibacterial activity and demonstrated a significant reduction in cytotoxicity. The impact of serum and initial investigations toward a mode of action highlight several features of this class of compounds as antibacterials. (C) 2005 Elsevier Ltd. All rights reserved.