硫色满酮并氮杂环衍生物体外抗真菌活性及构效关系研究  

Study on Antifungus Activities of Thiochromanon Nitrogen Heterocyclic Ring Derivatives in vitro and Their Structure-Activity Relationship

作　　者：郭兰弟[1] 贾苗辉[1] 杨更亮[1,2] 魏春亮[1] 管立[1] 马正月[1] 祝士国[1] 

机构地区：[1]河北大学药学院,河北保定071002 [2]中国科学院化学研究所分子科学中心

出　　处：《中国药师》2009年第1期15-17,共3页China Pharmacist

基　　金：河北省科技攻关项目(NO.06276479B;07276407D)

摘　　要：目的:对硫色满酮并氮杂环衍生物进行体外抗真菌实验,筛选具有抗真菌活性的化合物并探讨其构效关系。方法:利用微量稀释法,以氟康唑和两性霉素B为阳性对照药,测定硫色满酮类并氮杂环衍生物对白色念珠菌、新生隐球菌、断发毛癣菌、红色毛癣菌、申克孢子丝菌(菌丝相)、石膏样小孢子菌、卡氏枝孢霉、黑曲霉、絮状毛癣菌的体外抑菌活性。结果:Bb, Da,Db,I,K对絮状表皮癣菌抑制作用显著,尤其Db的MIC低于两性霉素B;K对石膏样小孢子丝菌的MIC与两性霉素B相当。二甲氨基和甲氧基取代后,抗真菌比其他取代基化合物抗真菌活性高。结论:硫色满酮并氮杂环衍生物对常见致病真菌有一定的体外抑菌活性,值得深入研究。To evaluate the activity of the thiochromanone derivatives against pathogenic fungus in vitro, flit the target compounds with antifugal activities and investigate their structure-activity relationship. Method： Compared with the positive control drug fluconazole and Amphotericin B, the susceptibilities of thiochromanone derivatives were evaluated in vitro by the method of microdilution. Candida albicans, Cryptococcus neofonnans, Trichophyton tonsurans, Triehophyton rubrum, Sporothrix schenckii （ hyphal form） , Microsporum gypseum, Cladosporium carrionii, Aspergillus niger and Epidermophyton floccosum were tested. Result： Bb, Da, Db, I, K has remarkable activties against Epidermophyton floccosum, especially Db which has a lower MIC than Amphotericin B; MIC of K against Microsporum gypseum was equivalent to Amphotericin B. dimethylamino and methoxy derivatives had better antifungal effect than others. Conclusion： The thiochromanone derivatives had certain antifugal activities against pathogenic fungus in vitro and deserved further research.

关 键 词：硫色满酮并氮杂环衍生物 致病性真菌 微量稀释法 体外抑菌活性 构效关系 

分 类 号：R965.1[医药卫生—药理学]