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

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.