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pleuromutilin antibiotics, pleuromutilin side effects
Pleuromutilin and its derivatives are antibacterial drugs that inhibit protein synthesis in bacteria by binding to the peptidyl transferase component of the 50S subunit of ribosomes

This class of antibiotics includes the licensed drugs retapamulin approved for topical use in humans, valnemulin and tiamulin approved for use in animals and the investigational drugs azamulin and lefamulin BC-3781


Pleuromutilin was first discovered as an antibiotic in 1950 It is derived from the fungus Clitopilus passeckerianus formerly Pleurotus passeckerianus, and has also been found in Drosophila subatrata, Clitopilus scyphoides, and some other Clitopilus species

Total synthesis

The total synthesis of pleuromutilin has been reported


  1. ^ Long, Katherine S; Lykke H Hansen; Lene Jakobsen; Birte Vester April 2006 "Interaction of Pleuromutilin Derivatives with the Ribosomal Peptidyl Transferase Center" PDF Antimicrobial Agents and Chemotherapy 50 4:1458–1462 doi:101128/AAC5041458-14622006 PMC 1426994  PMID 16569865 
  2. ^ Lolk, L; Pøhlsgaard, J; Jepsen, A S; Hansen, L H; Nielsen, H; Steffansen, S I; Sparving, L; Nielsen, A B; Vester, B; Nielsen, P 2008 "A Click Chemistry Approach to Pleuromutilin Conjugates with Nucleosides or Acyclic Nucleoside Derivatives and Their Binding to the Bacterial Ribosome" Journal of Medicinal Chemistry 51 16:4957–4967 doi:101021/jm800261u PMID 18680270 
  3. ^ Novak, R; Shlaes DM February 2010 "The pleuromutilin antibiotics:a new class for human use" Current Opinion in Investigational Drugs 11 2:182–91 PMID 20112168 
  4. ^ Kilaru, Sreedhar; Catherine M Collins; Amanda J Hartley; Andy M Bailey; Gary D Foster 2009-09-18 "Establishing Molecular Tools for Genetic Manipulation of the Pleuromutilin-Producing Fungus Clitopilus passeckerianus" Appl Environ Microbiol American Society for Microbiology 75 22:7196–7204 doi:101128/AEM01151-09 PMC 2786515  PMID 19767458 
  5. ^ Total synthesis of +--pleuromutilin E Grant Gibbons Journal of the American Chemical Society 1982 104 6, 1767-1769 doi:101021/ja00370a067
  6. ^ Synthetic studies directed toward naturally occurring cyclooctanoids 2 A stereocontrolled assembly of +--pleuromutilin via a remarkable sterically demanding oxy-Cope rearrangement Robert K Boeckman Jr, Dane M Springer, and Thomas R Alessi Journal of the American Chemical Society 1989 111 21, 8284-8286 doi:101021/ja00203a043
  7. ^ Fazakerley, N J, Helm, M D and Procter, D J 2013, Total Synthesis of +-Pleuromutilin Chem Eur J, 19:6718–6723 doi:101002/chem201300968
  8. ^ A modular and enantioselective synthesis of the pleuromutilin antibiotics Stephen K Murphy, Mingshuo Zeng, Seth B Herzon Science 02 Jun 2017:Vol 356, Issue 6341, pp 956-959 doi:101126/scienceaan0003

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