• Amphipathic Barbiturates as Mimics of Antimicrobial Peptides and the Marine Natural Products Eusynstyelamides with Activity against Multi-resistant Clinical Isolates 

      Paulsen, Marianne Hagensen; Engqvist, Magnus; Ausbacher, Dominik; Anderssen, Trude; Langer, Manuel Karl; Haug, Tor; Morello, Glenn Robert; Liikanen, Laura; Blencke, Hans-Matti; Isaksson, Johan; Juskewitz, Eric; Bayer, Annette; Strøm, Morten B. (Journal article; Tidsskriftartikkel; Peer reviewed, 2021-07-27)
      We report a series of synthetic cationic amphipathic barbiturates inspired by the pharmacophore model of small antimicrobial peptides (AMPs) and the marine antimicrobials eusynstyelamides. These N,N′-dialkylated-5,5-disubstituted barbiturates consist of an achiral barbiturate scaffold with two cationic groups and two lipophilic side chains. Minimum inhibitory concentrations of 2–8 μg/mL were achieved ...
    • Efficient and scalable synthesis of α,α-­disubstituted β-amino amides 

      Paulsen, Marianne Hagensen; Engqvist, Magnus; Ausbacher, Dominik; Strøm, Morten Bøhmer; Bayer, Annette (Journal article; Tidsskriftartikkel; Peer reviewed, 2016-07-12)
      A practical and efficient methodology for the preparation of 2-aminoethyl α,α-disubstituted β-amino amides in three steps from methyl cyanoacetate has been developed. The key step in the synthesis was the chemoselective reduction of the nitrile group in presence of an amide and aryl halide functionalities. Reduction with RANEY® Nickel catalyst, either with molecular hydrogen (8–10 bar) or under ...