Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety

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,...

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Detalles Bibliográficos
Autores principales: Shang, Ruofeng, Wang, Shengyu, Xu, Ximing, Yi, Yunpeng, Guo, Wenzhu, YuLiu, Liang, Jianping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2013
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3871055/
https://www.ncbi.nlm.nih.gov/pubmed/24376551
http://dx.doi.org/10.1371/journal.pone.0082595
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author Shang, Ruofeng
Wang, Shengyu
Xu, Ximing
Yi, Yunpeng
Guo, Wenzhu
YuLiu,
Liang, Jianping
author_facet Shang, Ruofeng
Wang, Shengyu
Xu, Ximing
Yi, Yunpeng
Guo, Wenzhu
YuLiu,
Liang, Jianping
author_sort Shang, Ruofeng
collection PubMed
description 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.
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spelling pubmed-38710552013-12-27 Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety Shang, Ruofeng Wang, Shengyu Xu, Ximing Yi, Yunpeng Guo, Wenzhu YuLiu, Liang, Jianping PLoS One Research Article 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. Public Library of Science 2013-12-23 /pmc/articles/PMC3871055/ /pubmed/24376551 http://dx.doi.org/10.1371/journal.pone.0082595 Text en © 2013 Shang et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Shang, Ruofeng
Wang, Shengyu
Xu, Ximing
Yi, Yunpeng
Guo, Wenzhu
YuLiu,
Liang, Jianping
Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety
title Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety
title_full Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety
title_fullStr Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety
title_full_unstemmed Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety
title_short Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety
title_sort chemical synthesis and biological activities of novel pleuromutilin derivatives with substituted amino moiety
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3871055/
https://www.ncbi.nlm.nih.gov/pubmed/24376551
http://dx.doi.org/10.1371/journal.pone.0082595
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