In their latest report the WHO warns “A post-antibiotic era — in which common infections and minor injuries can kill — far from being an apocalyptic fantasy, is instead a very real possibility for the 21st century”. Carbapenem antibiotics, e.g. meropenem, are usually the last line of defence against otherwise drug-resistant bacterial infections. However, the continuous evolution of bacteria possessing carbapenem-destroying enzymes – carbapenemases – threatens the utility of meropenem and related antibiotics. We aim to develop antibiotic resistance breakers that prevent the carbapenemases from destroying the last-line antibiotics and thereby revitalize the antibiotics for clinical use. Our group has identified several compound classes with potential to be developed to carbapenemase inhibitors. As part of the LacZyme group we have develop inhibitors through structure-based drug design and fragment-based approaches.
♦ Bioorg. Med. Chem., 2020, 115598. Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-β-lactamases. doi: 10.1016/j.bmc.2020.115598.
♦ Eur. J. Med.Chem. 2018, 634. A focused fragment library targeting the antibiotic resistance enzyme – Oxacillinase-48: synthesis, structural evaluation and inhibitor design. UiT´s open research archive;
♦ Eur. J. Med.Chem. 2017, 159. Metallo-β-lactamase inhibitors by bioisosteric replacement: preparation, activity and binding. UiT´s open research archive;