Blar i forfatter "Boomgaren, Marc"

Viser treff 1-3 av 3

    • Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor 

      Fjellaksel, Richard; Boomgaren, Marc; Sundset, Rune; Haraldsen, Ira Hebold; Hansen, Jørn H; Riss, Patrick (Journal article; Tidsskriftartikkel; Peer reviewed, 2017-08-14)
      In this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-<i>tert</i>-butylphenyl)-4-piperazinyl-benzimidazole scaffold <i>via</i> Cu-catalysed azide alkyne cycloaddition. Our main purpose was to find a more soluble compound based on the WAY207024 lead with nanomolar potency ...

    • Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-β-lactamases 

      Muhammad, Zeeshan; Skagseth, Susann; Boomgaren, Marc; Akhter, Sundus; Frøhlich, Christopher; Ismael, Aya; Christopeit, Tony; Bayer, Annette; Leiros, Hanna-Kirsti S. (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-06-18)
      Metallo-β-lactamases (MBLs) are an emerging cause of bacterial antibiotic resistance by hydrolysing all classes of β-lactams except monobactams, and the MBLs are not inhibited by clinically available serine-β-lactamase inhibitors. Two of the most commonly encountered MBLs in clinical isolates worldwide – the New Delhi metallo-β-lactamase (NDM-1) and the Verona integron-encoded metallo-β-lactamase ...

    • Two approaches to novel anticancer agents. Small-molecule library synthesis and evaluation 

      Boomgaren, Marc (Doctoral thesis; Doktorgradsavhandling, 2020-03-06)
      <p>The work presented in this dissertation combines two fully independent approaches to achieve compound libraries for anticancer drug research. <p>Project 1: Development of compounds inhibiting human dUTPase as an amplifier of a thymidylate synthase inhibitor based cancer therapy <p>The human dUTPase has received increased attention as a drug target in the recent years. Its inhibition can ...