2，3，3a，4．四氢硫色烯并[4，3-c]吡唑类化合物合成及其体外抗真菌活性研究  

Synthesis and Antifungal Activities in Vitro of 2,3,3a,4-Tetrahydrothiochromeno[4,3-c]pyrazole Derivatives

作　　者：马正月[1] 闫国英[2] 杨更亮[1] 祝士国[1] 管立[1] 

机构地区：[1]河北大学,药学院,河北保定071002 [2]河北大学,物理科学与技术学院,河北保定071002

出　　处：《中国药学杂志》2009年第8期630-633,共4页Chinese Pharmaceutical Journal

基　　金：河北科技攻关项目资金资助(07276407D和06276479B)

摘　　要：目的设计合成2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,并对其抗真菌活性进行初步评价。方法以取代苯硫酚为起始原料,首先合成中间体3-次苄基硫色满酮;然后利用水合肼和3-次苄基硫色满酮在醋酸中反应生成目标化合物。采用二倍稀释法对目标化合物的体外抗真菌活性进行测试。结果共合成了8个新的2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,并经过H-核磁共振、质谱和元素分析等确认了其结构。抗真菌活性实验结果表明,目标化合物对大部分供试真菌具有好的活性。结论2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物在体外具有抗真菌活性,有待深入研究。OBJECTIVE To design and synthesize 2, 3,3a, 4-tetrahydrothiochromeno[4, 3-c]pyrazole derivatives and measure their antifungal activity in vitro. METHODS The intermediate of 3-benzylidene-l-thiochromanones was synthesized from the substituted benzenethiols, secondly, the target compounds were obtained by the reactions of hydrazine with 3-benzylidene-l-thiochromanones in acetic acid. The antifungal activity of the target compounds in vitro was measured by consecutive double dilution. RESULTS Eight new 2, 3, 3a, 4-tetrahydrothiochromeno[4, 3-c]pyrazole derivatives were synthesized, and then their structures were identified by 1H-NMR, MS and elemental analysis. The result of antifungal activity indicated that the target compounds had good antifungal effects on most tested fungi. CONCLUSION 2, 3, 3a, 4-tetrahydrothiochromeno-[4, 3-c]pyrazole derivatives show antifungal activity in vitro, which required further research in the future.

关 键 词：硫色满酮 3-次苄基硫色满酮 微波辐射 抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学]