• Carbonylative Suzuki-Miyaura couplings of sterically hindered aryl halides: Synthesis of 2-aroylbenzoate derivatives 

      Ismael, Aya; Skrydstrup, Troels; Bayer, Annette (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-02-10)
      We have developed a carbonylative approach to the synthesis of diversely substituted 2-aroylbenzoate esters featuring a new protocol for the carbonylative coupling of aryl bromides with boronic acids and a new strategy to favour carbonylative over non-carbonylative reactions. Two different synthetic pathways – (i) the alkoxycarbonylation of 2-bromo benzophenones and (ii) the carbonylative Suzuki–Miyaura ...
    • A focused fragment library targeting the antibiotic resistance enzyme - Oxacillinase-48: Synthesis, structural evaluation and inhibitor design 

      Ahkter, Sundus; Lund, Bjarte Aarmo; Ismael, Aya; Langer, Manuel; Isaksson, Johan; Christopeit, Tony; Leiros, Hanna-Kirsti S.; Bayer, Annette (Journal article; Tidsskriftartikkel; Peer reviewed, 2018-02-10)
      β-Lactam antibiotics are of utmost importance when treating bacterial infections in the medical community. However, currently their utility is threatened by the emergence and spread of β-lactam resistance. The most prevalent resistance mechanism to β-lactam antibiotics is expression of β-lactamase enzymes. One way to overcome resistance caused by β-lactamases, is the development of β-lactamase ...
    • Method development towards synthesis of carbapenemase inhibitors 

      Ismael, Aya (Doctoral thesis; Doktorgradsavhandling, 2020-10-26)
      Carbapenemases are enzymes able to hydrolyze the last resort b-lactam antibiotics (carbapenems), which are used for the treatment of infections caused by resistant bacteria. Carbapenemases are structurally and mechanistically classified into serine-b-lactamases (SBLs) and metallo-b-lactamases (MBLs). In order to combat the hydrolytic activity of these enzymes, combination therapy of b-lactam with ...
    • Novel Synthesis of Lipoxine A4 Analogues. Towards Allostric Modulators for Human Cannabinoid Receptor Type 1 

      Ismael, Aya (Master thesis; Mastergradsoppgave, 2015-11-15)
      The synthesis of the benzoid-based lipoxine A4 (LXA4) is the focus of this study specifically, the para substituted benzoid system. LXA4 is an endogenous agonist binding with high affinity to (ALXR) receptor that initiate it to display anti-inflammatory and antioxidant activities. Arachidonic acid is the cascade of LXA4 and its derivatives. These compounds belong to the biological active eicosanoids, ...
    • Renewable Solvents for Palladium-Catalyzed Carbonylation Reactions 

      Ismael, Aya; Gevorgyan, Ashot; Skrydstrup, Troels; Bayer, Annette (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-09-04)
      Solvents constitute the largest component for many chemical processes and substitution of nonrenewable solvents is a longstanding goal for green chemistry. Here, we show that Pd-catalyzed carbonylative couplings, such as carbonylative cross-couplings, aminocarbonylations, and alkoxycarbonylations, can be successfully realized using renewable solvents. The present research covers not only well-established ...
    • 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 ...
    • Synthesis of aromatic lactone analogues of Lipoxin A4 

      Ismael, Aya; Zeeshan, Muhammad; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2022-02-09)
      Objective: Synthesis of novel aromatic Lipoxin A4 lactone analogues. <p><p>Results: Novel para-substituted aromatic lactone analogues of Lipoxin A4 have been synthesized in a convergent manner with six steps in the longest linear sequence in 12–13% yields, employing 2-deoxy-d-ribose as a chiral pool starting material and the classical E-selective Wittig olefnation.