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...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2014-11, Vol.19 (11), p.19050-19065
Main Authors: Shang, Ruo-Feng, Wang, Guan-Hua, Xu, Xi-Ming, Liu, Si-Jie, Zhang, Chao, Yi, Yun-Peng, Liang, Jian-Ping, Liu, Yu
Format: Article
Language:English
Subjects:
ADMET properties
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
antibacterial activity
Bacteria - drug effects
Diterpenes - chemical synthesis
Diterpenes - pharmacology
Electronic mail systems
Escherichia coli
Microbial Sensitivity Tests - methods
molecular docking
Molecular Docking Simulation
Pharmaceuticals
pleuromutilin derivatives
Pleuromutilins
Polycyclic Compounds
Public health
synthesis
Veterinary medicine
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Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules191119050