Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids

被引:14
作者
Jeong, Yong-Chul [1 ]
Anwar, Muhammad [1 ]
Moloney, Mark G. [1 ]
机构
[1] Univ Oxford, Chem Res Lab, Oxford OX1 3TA, England
关键词
Tetramate; Antibacterial; Enamine; TETRONIC ACIDS; ANTIBACTERIAL; DERIVATIVES; ANTIFUNGAL; DISCOVERY; INHIBITOR; BIOLOGY; POTENT; DOMAIN;
D O I
10.1016/j.bmcl.2014.03.013
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and evaluation of 3-enaminetetramic acids as antibacterial agents is reported; contrary to the analogous 3-acyltetramic acids, the enaminetetramic acid class of compound exhibits modest antibacterial activity against a limited spectrum of organisms, and even that activity is strongly dependent on the identity of the tetramate ring substituents. Moreover, these compounds appear to have a different mode of action to the analogous 3-acyltetramic acids, and appear to offer more limited opportunity for further elaboration in drug discovery. Crown Copyright (c) 2014 Published by Elsevier Ltd. All rights reserved.
引用
收藏
页码:1901 / 1906
页数:6
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