截短侧耳素类化合物的研究进展  

Research progress on pleuromutilin and its derivatives

作　　者：杨冠洲[1] 尚若锋[2] 

机构地区：[1]兰州大学药学院,兰州730020 [2]中国农业科学院兰州畜牧与兽药研究所,兰州730050

出　　处：《南方农业学报》2015年第8期1527-1532,共6页Journal of Southern Agriculture

基　　金：中央级科研院所科技基础性工作专项资金项目(1610322014003)

摘　　要：截短侧耳素是20世纪50年代从高等真菌中分离获得的一种具有抗菌活性的双萜类化合物,其抗菌活性较弱、水溶性较差,但通过分子结构改造可获得具有良好抗阳性耐药菌活性的截短侧耳素类及其衍生类药物。文章就截短侧耳素类药物、抗菌机理、耐药机理及近5年合成的截短侧耳素类衍生物进行全面综述,发现当前通过化学修饰截短侧耳素类化合物侧链而筛选获得有效的截短侧耳素类候选药物或兽用药物仍较少。因此,今后应根据截短侧耳素类化合物侧链结构与生物活性的关系,进行合理的分子结构设计,通过化学合成手段及生物活性、稳定性与毒理学等研究,筛选出更多的截短侧耳素类候选药物,从而创制出更多高效、安全的新型截短侧耳素类兽用药物。Pleuromutilin was diterpene with antibacterial activities, which was isolated from higher fungi in the 1950 s.However, because of its low antibacterial activities and solubility, new derivatives and derivative drugs with high activity against drug-resistant Gram-positive bacteria could be obtain by modifying its structure. The present study was conducted to summarize comprehensively pleuromutilin drugs, and their antibacterial and drug-resistant mechanisms, as well as their novel synthesized derivatives. The results showed that, there were still few effective candidate or veterinary drugs which were obtained by modifying side chain of pleuromutilin. Therefore, the future works should focus on designing rational structure based on structure-activity relationship. By chemical synthesis and studies on bioactivity, stability and toxicology, more novel veterinary drugs of pleuromutilin with high activities and safety were screened out.

关 键 词：截短侧耳素 衍生物 化学修饰 抑菌机理 耐药机理 抗菌活性 

分 类 号：S859.796[农业科学—临床兽医学]