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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Research Article

Synthesis and Antibacterial Activity Against MRSA of Pleuromutilin Derivatives Possessing a Mercaptoethylamine Linker

Author(s): Zhao-Sheng Zhang, Yun-Zhen Huang, Jian Luo, Bing-Feng Wang, Zhen Jin, Ya-Hong Liu and You-Zhi Tang*

Volume 14, Issue 6, 2018

Page: [585 - 594] Pages: 10

DOI: 10.2174/1573406414666180416131737

Price: $65


Background: Methicillin resistant Staphylococcus aureus (MRSA) usually invalidate powerful antibiotics in the clinic. Pleuromutilin derivatives have been reported to possess antibacterial activity against MRSA.

Objective: The antibacterial activities against MRSA of a series of thirteen synthetic pleuromutilin derivatives were investigated through in vitro models.

Methods: A series of novel thioehter pleuromutilin derivatives incorporating various aromatic substituents into the C14 side chain have been reported. The in vitro antibacterial activities of these derivatives against MRSA and Escherichia coli were tested by the broth dilution method.

Results: Twelve pleuromutilin derivatives were designed, synthesized and evaluated for in vitro antibacterial activities against four Staphylococcus aureus strains. From structure-activity relationship studies, compound 11c was identified as promising compounds with the most potent in vitro antibacterial activity among the series (MIC = 0.0625-0.125 µg/ml) against Staphylococcus aureus strains. The binding of compound 11c to the 50s ribosome was investigated by molecular modeling.

Conclusion: It was found that there is a reasonable correlation between the binding free energy and the antibacterial activity.

Keywords: Antibacterial activity, antibiotics, antibacterial Activity, pleuromutilin, MRSA, molecular docking.

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