One-pot synthesis and biological evaluation of aspergillamides and analogues

Barbara Beck, Sibylle Hess, Alexander Dömling

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A one-pot total synthesis of aspergillamide and analogues by a solution phase Ugi multi component reaction (MCR) is described. The reaction is easily performed in 96-well plates and offers a facile access to diverse aspergillamide analogue compound libraries. The antibiotic and cytotoxic activity of these compounds is measured. Several of them are more potent than the natural product. (C) 2000 Elsevier Science Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)1701-1705
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number15
Publication statusPublished - 7-Aug-2000


  • amide
  • aspergillamide
  • drug analog
  • unclassified drug
  • antibacterial activity
  • antifungal activity
  • article
  • Bacillus subtilis
  • Candida albicans
  • cell proliferation
  • drug inhibition
  • drug screening
  • drug synthesis
  • nonhuman
  • Pseudomonas aeruginosa
  • Staphylococcus aureus
  • tumor cell line

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