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Molecules 2014, 19(11), 19050-19065; doi:10.3390/molecules191119050

Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents

1
Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Ministry of Agriculture, Lanzhou 730050, China
2
School of Public Health, Lanzhou University, Lanzhou 730000, China
3
Department of Toxicology, School of Public Health, Guiyang Medical University, Guiyang 550004, China
4
College of Chemical Engineering, Shijiazhuang University, Shijiazhuang 050035, China
*
Authors to whom correspondence should be addressed.
Received: 23 October 2014 / Revised: 11 November 2014 / Accepted: 12 November 2014 / Published: 19 November 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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. View Full-Text
Keywords: pleuromutilin derivatives; antibacterial activity; synthesis; molecular docking; ADMET properties pleuromutilin derivatives; antibacterial activity; synthesis; molecular docking; ADMET properties
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Shang, R.-F.; Wang, G.-H.; Xu, X.-M.; Liu, S.-J.; Zhang, C.; Yi, Y.-P.; Liang, J.-P.; Liu, Y. Synthesis and Biological Evaluation of New Pleuromutilin Derivatives as Antibacterial Agents. Molecules 2014, 19, 19050-19065.

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