State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai, China.
Bioorg Med Chem Lett. 2013 Jul 1;23(13):3697-9. doi: 10.1016/j.bmcl.2013.05.023. Epub 2013 May 17.
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.
设计并合成了一系列带有 3-三唑甲基或 3-羧酰胺侧链的苯并恶嗪基恶唑烷酮，旨在开发具有改良性能的抗菌剂。对这些新型化合物进行了体外抗革兰氏阳性菌活性评估，涵盖了一系列耐药和敏感菌。大多数带有 3-三唑甲基的类似物表现出良好至中等的抗菌活性。化合物 12a 对所有测试菌株的活性比利奈唑胺提高了四倍，这表明它是一种有前途的抗菌剂，值得进一步评估。
