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Chemical synthesis and biological activities of novel pleuromutilin derivatives with substituted amino moiety.

ABSTRACT: Novel pleuromutilin derivatives designed based on the structure of valnemulin were synthesized and evaluated for their in vitro antibacterial activities. These pleuromutilin derivatives with substituted amino moiety exhibited excellent activities against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae. Compound 5b showed the highest antibacterial activities and even exceeded tiamulin. Moreover, the docking experiments provided information about the binding model between the synthesized compounds and peptidyl transferase center (PTC) of 23S rRNA.

SUBMITTER: Shang R 

PROVIDER: S-EPMC3871055 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature

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Chemical synthesis and biological activities of novel pleuromutilin derivatives with substituted amino moiety.

Shang Ruofeng R   Wang Shengyu S   Xu Ximing X   Yi Yunpeng Y   Guo Wenzhu W   Yuliu   Liang Jianping J  

PloS one 20131223 12

Novel pleuromutilin derivatives designed based on the structure of valnemulin were synthesized and evaluated for their in vitro antibacterial activities. These pleuromutilin derivatives with substituted amino moiety exhibited excellent activities against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae. Compound 5b showed the highest antibacterial activities and even exceeded tiamulin. Moreover, the dock  ...[more]

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