新型3-氨基-2-唑恶唑烷酮类化合物的合成及群体感应抑制活性评价  

Synthesis and evaluation of new 3-aminooxazolidin-2-one derivatives for inhibiting bacterial quorum sensing

作　　者：曾善超 宋宏锐[1] 肖军海[2] 

机构地区：[1]沈阳药科大学制药工程学院,沈阳110016 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《国际药学研究杂志》2016年第3期476-480,共5页Journal of International Pharmaceutical Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2014ZX09507-009-018)

摘　　要：目的发展具有群体感应(QS)抑制活性的3-氨基-2-吃恶唑烷酮类化合物。方法以2-肼基乙醇为原料,经过环合,缩合,水解再缩合的方法合成了一系列以3-氨基-2-吃恶唑烷酮为母核的化合物。并对目标化合物进行紫色色杆菌QS抑制活性评价。结果本研究得到目标化合物8个,结构均经1H NMR、MS确证。生物活性评价结果表明,化合物Z2对紫色色杆菌QS有抑制活性。结论所合成的化合物均未见文献报道,合成路线简单稳定可靠。化合物Z2对QS有一定的抑制活性。Objective To develop some 3-aminooxazolidin-2-one derivatives with bacteria quorum sensing（QS）inhibitory activity. Methods Using（2-hydroxyethyl）hydrazine as raw material,we finished the synthesis through cyclization,condensation,hydrolysis and condensation reaction,and evaluated their inhibition of QS via Chromobacterium violaceum. Results Eight compounds were synthesized and their structures were confirmed by1 H NMR and MS characterization. Compounds Z2 had inhibitory effect against QS. Conclusion None of the eight synthesized compounds have been reported before and the synthetic route is reliable. Compounds Z2 have inhibitory effect against QS.

关 键 词：细菌群体感应 3-氨基-2-吃恶唑烷酮 抑制活性 

分 类 号：R914.5[医药卫生—药物化学]