Structure-activity relations of azafluorenone and azaanthraquinone as antimicrobial compounds
Structure-activity relations of azafluorenone and azaanthraquinone as antimicrobial compounds
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DOI：
10.1016/j.bmcl.2004.12.059
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发表时间：
2005-02-15
影响因子：
2.7
通讯作者：
Taniguchi, M
中科院分区：
文献类型：
--
作者：
Koyama, J;Morita, I;Taniguchi, M
测定了2个氮杂荧酮类化合物、4个1-氮杂并蒽醌类化合物、5个2-氮杂并蒽醌类化合物和1个2-氮杂喹酮类化合物的抗菌活性。几种氮杂蒽醌具有广泛而有效的活性，而氮杂二茂酮则表现出较弱的活性。其构效关系如下：(1)活性按2-氮杂蒽醌>、1-氮杂蒽醌>、氮杂二茂酮的顺序递减；(2)羧基上的羟基增强活性。此外，还讨论了还原电位、疏水参数和抗菌活性之间的关系。(C)2005爱思唯尔有限公司。保留所有权利。
Antimicrobial activities of two azafluorenones, four 1-azaanthraquinones, five 2-azaanthraquinones, and one 2-azaquinone were tested. Several azaanthraquinones possessed broad, potent activity, while the azafluorenones demonstrated weak activity. The following structure-activity relationship was postulated: (1) activity decreased in the order 2-azaanthraquinones >1-azaanthraquinones > azafluorenones; and (2) a hydroxyl group at the peri-carbonyl group enhanced activity. In addition, correlations among reduction potential, hydrophobic parameter, and antimicrobial activity were discussed. (C) 2005 Elsevier Ltd. All rights reserved.