3-硝基-2H-色烯衍生物的合成及抗菌活性研究  

Synthesis and evaluation of 3-nitro-2H-chromene derivatives as new antibacterials

作　　者：肖国强[1] 殷霞[1] 胡志鹏[1] 鄢明[1] 

机构地区：[1]中山大学药学院,广东广州510006

出　　处：《华西药学杂志》2012年第3期235-237,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:21172270);珠海市科技计划资助项目(PC20081006)

摘　　要：目的设计并合成一系列3-硝基-2H-色烯衍生物,研究其抗菌活性与构效关系。方法以水杨醛和2-硝基乙醇为原料合成目标化合物,采用肉汤稀释法测定抗菌活性。结果目标化合物结构均经过1HNMR和HRMS确证,3-硝基-2H-色烯衍生物对金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌具有很好的抑制活性(MIC=4μg·mL-1)。结论 3-硝基-2H-色烯衍生物具有进一步深入研究的价值。OBJECTIVE To design and synthesize a series of 3-nitro-2H-chromene derivatives and their analogs,and to evaluate their antibacterial activities and structure-activity relationship.METHODS The target compounds were synthesized from salicylaldehydes and 2-nitroethanol.Their antibacterial activities were tested against a panel of Gram-positive and Gram-negative pathogens through broth microdilution method.RESULTS The structures of all new compounds were characterized by 1HNMR and HRMS.3-Nitro-2H-chromene derivatives showed potent antibacterial activities（MIC = 4 μg·mL-1） against S.aureus and methicillin resistant S.aureus.CONCLUSION 3-Nitro-2H-chromene is a valuable antibacterial pharmacophore for further studies.

关 键 词：3-硝基-2H-色烯衍生物 合成 抗菌活性 定量构效关系 

分 类 号：R914[医药卫生—药物化学]