Abstract

A series of novel pleuromutilin derivatives were designed and synthesized based on the twin drugs theory. Piperazinyl and thioether were used as the linkage to connect the pleuromutilin nuclear and sulfonamide to improve the biological activity and water solubility of derivatives. The in vitro antibacterial activities against drug-sensitive and drug-resistance bacteria were evaluated by agar dilution method. Most of the 25 compounds displayed excellent antibacterial activities against drug-sensitive bacteria, particularly, five compounds (9, 10, 11, 14a and 14b) exerted the excellent antibacterial activities against drug-resistance bacteria.

中文翻译：

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双药理论截短侧耳素衍生物的设计、合成及抗菌活性评价

 抽象的

基于双药理论设计合成了一系列新型截短侧耳素衍生物。以哌嗪基和硫醚为键连接截短侧耳素核和磺酰胺，提高衍生物的生物活性和水溶性。采用琼脂稀释法评价其对药物敏感菌和耐药菌的体外抗菌活性。 25个化合物中的大多数对药物敏感菌表现出优异的抗菌活性，特别是5个化合物（9、10、11、14a和14b ）对耐药菌表现出优异的抗菌活性。