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3-溴-4-硫色(满)酮衍生物的合成及其抗真菌活性研究

Syntheses and the antifungal activity of 3-bromo-4-thiochrom(an)ones

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【作者】 齐平靳颖华郭春方林

【Author】 QI Ping 1,JIN Ying-hua 1,GUO Chun 2,FANG Lin 2 (1.Department of Pharmacy,The General Hospital of the Beijing Military Command,Beijing 100700,China;2.School of Pharmceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China)

【机构】 北京军区总医院药剂科沈阳药科大学制药工程学院沈阳药科大学制药工程学院 北京100700北京100700辽宁沈阳110016辽宁沈阳110016

【摘要】 目的设计合成 3 溴 4 硫色 (满 )酮类化合物 ,并对其抗真菌活性进行初步评价。方法以取代硫色 (满 )酮为原料 ,经溴化、氧化等反应制得目标化合物 ,化合物的体外抗真菌活性测定采用二倍浓度稀释法。结果共合成了 9个未见文献报道的新化合物 ,经红外光谱、核磁共振氢谱及元素分析确证其结构。其中化合物Ⅴb 的活性好于或相当于对照药。结论硫色 (满 )酮 3 位溴取代后具有较强的抗真菌活性。

【Abstract】 Aim To design and synthesize the 3-bromo-4-thiochrom(an)ones,and to value their antifungal activity. Methods BZ] The target compounds were prepared from the thiochromanones through bromination and oxidation,their antifungal effects were tested in vitro . Results Nine new compounds were synthesized.The structures of these compounds were confirmed by IR, 1H-NMR and elemental analyses.The compound The target compounds were prepared from the thiochromanones through bromination and oxidation,their antifungal effects were tested in vitro . Results Nine new compounds were synthesized.The structures of these compounds were confirmed by IR, 1H-NMR and elemental analyses.The compound Ⅴ_b exhibited excellent antifungal activity.Its MIC value was below or equal to that of the control. Conclusion The 3-bromo substituted thiochromanones show potent antifungal activity.

  • 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2003年04期
  • 【分类号】R914
  • 【被引频次】17
  • 【下载频次】199
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