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Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents
Several pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the derivatives against methicillin-resistant S. aureus, methicillin-resistant S. epidermidis, S. aureus, S. epidermidis, E. coli...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271455/ https://www.ncbi.nlm.nih.gov/pubmed/25415471 http://dx.doi.org/10.3390/molecules191119050 |
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author | Shang, Ruo-Feng Wang, Guan-Hua Xu, Xi-Ming Liu, Si-Jie Zhang, Chao Yi, Yun-Peng Liang, Jian-Ping Liu, Yu |
author_facet | Shang, Ruo-Feng Wang, Guan-Hua Xu, Xi-Ming Liu, Si-Jie Zhang, Chao Yi, Yun-Peng Liang, Jian-Ping Liu, Yu |
author_sort | Shang, Ruo-Feng |
collection | PubMed |
description | Several pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the derivatives against methicillin-resistant S. aureus, methicillin-resistant S. epidermidis, S. aureus, S. epidermidis, E. coli, and B. cereus were tested by the agar dilution method and Oxford cup assay. All the screened compounds displayed potent activity. Compound 6d was the most active antibacterial agent because of its lowest MIC value and largest inhibition zone. Docking experiments were performed to understand the possible mode of the interactions between the derivatives and 50S ribosomal subunit. Moreover, the absorption, distribution, metabolism, excretion and toxicity properties of the synthesized compounds were analyzed after prediction using the Advanced Chemistry Development/Percepta Platform available online. |
format | Online Article Text |
id | pubmed-6271455 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62714552019-01-07 Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents Shang, Ruo-Feng Wang, Guan-Hua Xu, Xi-Ming Liu, Si-Jie Zhang, Chao Yi, Yun-Peng Liang, Jian-Ping Liu, Yu Molecules Article Several pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the derivatives against methicillin-resistant S. aureus, methicillin-resistant S. epidermidis, S. aureus, S. epidermidis, E. coli, and B. cereus were tested by the agar dilution method and Oxford cup assay. All the screened compounds displayed potent activity. Compound 6d was the most active antibacterial agent because of its lowest MIC value and largest inhibition zone. Docking experiments were performed to understand the possible mode of the interactions between the derivatives and 50S ribosomal subunit. Moreover, the absorption, distribution, metabolism, excretion and toxicity properties of the synthesized compounds were analyzed after prediction using the Advanced Chemistry Development/Percepta Platform available online. MDPI 2014-11-19 /pmc/articles/PMC6271455/ /pubmed/25415471 http://dx.doi.org/10.3390/molecules191119050 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Shang, Ruo-Feng Wang, Guan-Hua Xu, Xi-Ming Liu, Si-Jie Zhang, Chao Yi, Yun-Peng Liang, Jian-Ping Liu, Yu Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents |
title | Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents |
title_full | Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents |
title_fullStr | Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents |
title_full_unstemmed | Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents |
title_short | Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents |
title_sort | synthesis and biological evaluation of new pleuromutilin derivatives as antibacterial agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271455/ https://www.ncbi.nlm.nih.gov/pubmed/25415471 http://dx.doi.org/10.3390/molecules191119050 |
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