Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents
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新型苯并恶嗪基恶唑烷酮类潜在抗菌剂的合成及生物学评价
DOI：
10.1016/j.bmcl.2013.05.023
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发表时间：
2013-07-01
影响因子：
2.7
通讯作者：
Yang, Yushe
中科院分区：
文献类型：
--
作者：
Guo, Bin;Fan, Houxing;Yang, Yushe
设计合成了一系列含3-三唑甲基或3-甲酰胺侧链的苯并恶嗪基恶唑烷酮类化合物，旨在开发性能更好的抗菌剂。在体外抗菌活性的这些新的化合物进行了评价对一组耐药和敏感的革兰氏阳性菌。大多数3-三唑基甲基的类似物显示出良好的至中等的抗菌活性。与利奈唑胺相比，化合物12 a对所有测试菌株的活性均表现出四倍的增加，其被鉴定为有前途的抗菌剂以用于进一步评价。(C)2013爱思唯尔有限公司保留所有权利。
A number of benzoxazinyl-oxazolidinones bearing 3-trizolylmethyl or 3-carboxamide side chain were designed and synthesized with the aim to develop antibacterial agents with improved properties. In vitro antibacterial activities of these novel compounds were evaluated against a panel of resistant and susceptible Gram-positive bacteria. Most analogues bearing 3-trizolylmethyl showed good to moderate antibacterial activities. Compound 12a exhibited a fourfold increase in activity compared with linezolid against all the tested strains, which was identified to be a promising antibacterial agent for further evaluation. (C) 2013 Elsevier Ltd. All rights reserved.