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Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens

文献类型：期刊论文

作者Fu, Liqiang; Jiang, Zhiteng; Cai, Zhan; Liu, Xin; He, Huili; Yang, Yushe
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2009-09-15
卷号19期号:18页码:5407-5410
关键词Pleuromutilin Gram-positive bacteria Water-soluble phosphate prodrugs
ISSN号0960-894X
DOI10.1016/j.bmcl.2009.07.115
文献子类Article
英文摘要A phosphate prodrug strategy was investigated to address the problem of poor aqueous solubility of pleuromutilin analogues. Water-soluble phosphate prodrugs 6a, 6b and 6c of pleuromutilin analogues were designed and synthesized. Three compounds all exhibited excellent aqueous solubility (>50 mg/mL) at near-neutral pH and sufficient stability in buffer solution. In particular, the phenol pleuromutilin prodrug 6c displayed favourable pharmacokinetic profiles and comparable potency with vancomycin against MSSA and MRSA strains in vivo. (C) 2009 Elsevier Ltd. All rights reserved.
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000269760900027
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/279130]  
专题药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Yang, Yushe
作者单位Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai Inst Biol Sci, Shanghai 20103, Peoples R China
推荐引用方式
GB/T 7714		 Fu, Liqiang,Jiang, Zhiteng,Cai, Zhan,et al. Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(18):5407-5410.
APA Fu, Liqiang,Jiang, Zhiteng,Cai, Zhan,Liu, Xin,He, Huili,&Yang, Yushe.(2009).Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(18),5407-5410.
MLA Fu, Liqiang,et al."Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.18(2009):5407-5410.

入库方式： OAI收割

来源：上海药物研究所

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