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Molecules 2017, 22(6), 996;

Synthesis and Biological Activity Evaluation of Novel Heterocyclic Pleuromutilin Derivatives

Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Ministry of Agriculture, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Lanzhou 730050, China
Author to whom correspondence should be addressed.
Received: 6 May 2017 / Revised: 8 June 2017 / Accepted: 13 June 2017 / Published: 15 June 2017
(This article belongs to the Section Medicinal Chemistry)
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A series of pleuromutilin derivatives were synthesized by two synthetic procedures under mild reaction conditions and characterized by Nuclear Magnetic Resonance (NMR), Infrared Spectroscopy (IR), and High Resolution Mass Spectrometer (HRMS). Most of the derivatives with heterocyclic groups at the C-14 side of pleuromutilin exhibited excellent in vitro antibacterial activities against Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphylococcus epidermidis (MRSE), and vancomycin-resistant Enterococcus (VRE) in vitro antibacterial activity. The synthesized derivatives which contained pyrimidine rings, 3a, 3b, and 3f, displayed modest antibacterial activities. Compound 3a, the most active antibacterial agent, displayed rapid bactericidal activity and affected bacterial growth in the same manner as that of tiamulin fumarate. Moreover, molecular docking studies of 3a and lefamulin provided similar information about the interactions between the compounds and 50S ribosomal subunit. The results of the study show that pyrimidine rings should be considered in the drug design of pleuromutilin derivatives. View Full-Text
Keywords: pleuromutilin derivatives; antibacterial activity; synthesis; molecular docking pleuromutilin derivatives; antibacterial activity; synthesis; molecular docking

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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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Yi, Y.; Fu, Y.; Dong, P.; Qin, W.; Liu, Y.; Liang, J.; Shang, R. Synthesis and Biological Activity Evaluation of Novel Heterocyclic Pleuromutilin Derivatives. Molecules 2017, 22, 996.

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