Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety

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• 作者：Yunpeng Yi^a ; ^b ; Ximing Xu^c ; Yu Liu^a ; ^b ; Shuijin Xu^d ; Xin Huang^a ; ^b ; Jianping Liang^a ; ^b ; ^{liangjp1963@163.com} ; Ruofeng Shang^a ; ^b ; ^{shangrf1974@163.com}
• 关键词：Pleuromutilin derivatives ; Synthesis ; Antibacterial activity ; Molecular docking
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：687-695
• 全文大小：1745 K
• 卷排序：126

文摘

A series of novel pleuromutilin derivatives with substituted pyrimidine moieties were synthesized. Synthesized compounds were evaluated for their antibacterial activity. Compounds 3 and 5h showed excellent antibacterial activity. Compounds 3 displayed rapid actericidal activity and potent therapeutic efficacy in mouse systemic infection.