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Development of metallo-β-lactamase inhibitors to control antibioticresistance
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Organic Chemistry. (Mate Erdelyi)
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Organic Chemistry. (Mate Erdelyi)ORCID iD: 0000-0003-3798-3322
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Organic Chemistry. (Mate Erdelyi)ORCID iD: 0000-0003-0359-5970
2018 (English)Conference paper, Poster (with or without abstract) (Refereed)
Abstract [en]

According to the recent reports of WHO,1 one of the major challenges of the XXI century isthe rapidly growing bacterial resistance against antibiotics. As a result, bacterial infectionsmay become untreatable within a considerable time giving simple infections, such aspneumonia or Septicemia, a highly probable mortal prognosis. Without access to efficientantibiotics simple surgeries, giving birth and dental interventions, for example, may becomerisky.The mostly widely spread mechanism of bacterial resistance is mediated by β-lactamases, aspecific group of enzymes responsible for the degradation or modification of antibiotics priorto reaching their bacterial target sites. Metallo-β-lactamases are the clinically mostimportant, as these cleave also carbapenems, which are the last resort antibiotics to date.Recent reports indicate that bacteria need barely three months to develop resistance againstnew antibiotics, making their development into an unattractive, high risk approach.The key point of the mechanism of antibiotics degradation by metallo-β-lactamases is thecreation of a tetrahedral intermediate (EI) upon a C–N bond cleavage (Fig. 1). This stepinvolves irreversible chemical changes, which lead to the inactivation of the β-lactamantibiotics.

This project is focused on the development of bioisosters of existing antibiotics, i.e.compounds resembling the transition state of their cleavage (Fig 1). These are expected tohave both metallo-β-lactamase inhibitory and antibiotic properties. This strategy allows forthe reactivation of existing antibiotics, and possibly the avoidance of the need forcombinatorial therapy.Further studies of interaction between NDM-1 (New Delhi Metallo-β-Lactamases-1) andsynthesized ligands will bring insights immensely valuable for the prevention of bacterialresistance against antibiotic treatment.

Place, publisher, year, edition, pages
2018.
National Category
Chemical Sciences
Research subject
Chemistry with specialization in Organic Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-357813OAI: oai:DiVA.org:uu-357813DiVA, id: diva2:1240489
Conference
1ST NATIONAL MEETING OF THE SWEDISH CHEMICAL SOCIETY in Lund, 17-20 June 2018
Available from: 2018-08-21 Created: 2018-08-21 Last updated: 2018-08-21

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Andersson, HannaErdélyi, Máté

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