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

Synthesis of 2,3,3a,4-tetrahydrothiochromenopyrazoles derivatives and their antifungal activity in vitro

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

机构地区：[1]河北大学药学院,河北省药物质量研究重点实验室,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：《中国药物化学杂志》2008年第3期170-174,205,共6页Chinese Journal of Medicinal Chemistry

基　　金：河北省科技攻关项目(07276407D06276479B)

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,并对其体外抗真菌活性进行初步评价。方法以取代苯硫酚为起始原料,合成中间体3-次苄基硫色满酮,该中间体与水合肼在热醋酸中反应生成目标化合物。采用二倍稀释法对4种受试真菌——絮状表皮毛癣菌(E.floccosum)、石膏样小孢子菌(M.gypse-um)、绿色木霉菌(T.viride)和断发毛癣菌(T.tonsurans)进行体外抗真菌活性测试。结果合成了12个新的2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,其结构经氢核磁共振谱、质谱和元素分析确证。抗真菌实验结果表明,所合成的目标化合物对供试真菌具有一定程度的抑制活性。结论2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物具有体外抗真菌活性。Aim To synthesize 2, 3, 3a, 4- tetrahydrothiochromeno [ 4, 3-c ] pyrazoles derivatives and measure their antifungal activity. Methods Substituted benzenethiols were used as starting materials. Firstly they were transformed into 3-arylidene-1-thiochromanones. Secondly the target compounds were prepared by the condensation of hydrazine with the intermediates in hot acetic acid. And their antifungal activity was tested by consecutive double dilution for E. floccosurn, M. gypseum, T. viride, and T. tonsurans. Results Twelve new 2, 3, 3a, 4-tetrahydrothioehromeno [ 4, 3-c ] pyrazoles derivatives were synthesized, and their structures were conformed by 1^H-NMR, MS and element analysis. The result of antifungal experiment indicated that the target compounds had good antifungal effect on most tested fungi in vitro. Conclusion 2, 3, 3a, 4-tetrahydrothiochromeno[4, 3-c]pyrazoles derivatives showed certain antifungal activity in vitro.

关 键 词：硫色满酮 3-次苄基硫色满酮 水合肼 微波辐射 

分 类 号：R914[医药卫生—药物化学]