氯代硫色烯并[4,3-c]吡唑啉衍生物的合成及其抗真菌活性  

Synthesis and antifungal activity of chlorobenzothiopyrano[4,3-c]pyrazolines

作　　者：祝士国[1] 杨更亮[1] 马正月[1] 魏春亮[1] 郭兰弟[1] 

机构地区：[1]河北大学药学院,保定071002

出　　处：《中国新药杂志》2008年第12期1034-1036,共3页Chinese Journal of New Drugs

基　　金：河北省科技攻关项目(07276407D,06276479B);国家自然科学基金资助项目(20375010)

摘　　要：目的:设计合成氯代硫色烯并[4,3-c]吡唑啉衍生物,并考察其抗真菌活性。方法:以对氯苯硫酚为原料经多步反应合成目标化合物,并采用柱色谱实现其顺反异构体的分离。结果:合成6个未见文献报道的新化合物,其结构均经核磁共振氢谱、质谱确证。初步药理实验显示目标化合物具有较强的抗真菌活性。结论:氯代硫色烯并[4,3-c]吡唑啉衍生物在体外具有一定的抗真菌活性。Objective ： To design and synthesize chlorobenzothiopyrano [ 4,3-c ] pyrazolines, and to determine their antifungal activities. Methods： The target compounds were synthesized in several steps starting from 4- chlorobenzenethiol. Trans- and cis-diastereomers were separated by column chroamtography. Results： Six new compounds were synthesized. All of them were confirmed by 1H-NMR and MS. Preliminary pharmacological test showed that the target compounds possessed potent antifungal activity. Conclusion： The synthesized chlorobenzo- thiopyrano[ 4,3-c ] pyrazolines have an in vitro antifungal activity in some tested fungal strains.

关 键 词：对氯苯硫酚 硫色烯并[4 3-c]吡唑啉 抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学] R965.1[医药卫生—药学]