截短侧耳素类衍生物的研究现状与发展趋势  

Research and development tendency of pleuromutilin derivatives

作　　者：凡媛 周宇航 王洛菊 尚若锋[1] FAN Yuan;ZHOU Yuhang;WANG Luoju;SHANG Ruofeng(Key Lab of New Animal Drug Project,Gansu Province,Key Lab of Veterinary Pharmaceutical Development,Ministry of Agriculture and Rural Affairs,Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS,Lanzhou Gansu 730050,China;Shandong Qilu King-Phar Pharmaceutical Co.,LTD.,Pingyin Shangdong 250400,China)

机构地区：[1]中国农业科学院兰州畜牧与兽药研究所农业农村部兽用药物创制重点实验室甘肃省新兽药工程重点实验室,甘肃兰州730050 [2]山东齐发药业有限公司,山东平阴250400

出　　处：《中兽医医药杂志》2021年第5期29-37,共9页Journal of Traditional Chinese Veterinary Medicine

基　　金：“泉城学者”建设工程项目(00252019025)。

摘　　要：截短侧耳素及其衍生物具有良好的抗菌活性和不易产生交叉耐药性等优点,已成为国际上的研究热点。通过对截短侧耳素C-14位侧链修饰,已成功研发出两种兽用药物和两种人用药物,完全实现了从兽用跨越到人用的领域,表现出优越的临床应用前景。本文对近几年C-14位侧链含不同芳香环基团的截短侧耳素类衍生物及其抑菌活性进行了全面综述,以期为今后创制更多的截短侧耳素类药物提供参考。Pleuromutilin and its derivatives have become a research hot topic in the world because of their high antibacterial activity and low cross-resistance. The modification of pleuromutilin side chain has led to two veterinary drugs and two human drugs, and thus completely realized the leap from veterinary to human use, displaying superior clinical prospects. In this review, the novel pleuromutilin derivatives bearing different aromatic ring at the C-14 side chain, as well as their antibacterial activities which were reported in recent years, were comprehensively reviewed for providing a useful help to develop more pleuromutilin drugs.

关 键 词：截短侧耳素 抑菌活性 化学修饰 抑菌机理 耐药机理 

分 类 号：S859.7[农业科学—临床兽医学]