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dc.contributor.advisorBayer, Annette
dc.contributor.advisorLeiros, Hanna-Kirsti
dc.contributor.advisorIsmael, Aya
dc.contributor.authorMagnussen, Harald
dc.date.accessioned2021-10-04T05:45:12Z
dc.date.available2021-10-04T05:45:12Z
dc.date.issued2020-06-01en
dc.description.abstractAntibiotic resistance is threatening the achievements of modern medicine and will evidentially lead to a situation, in which we stand helpless against common bacterial infections. The largest and most widely used group of antibiotics are the β-lactams. One of the major resistance determinants against β-lactam antibiotics is the expression of hydrolytic enzymes, called β-lactamases (BLs). The main concern of BLs is that they are threatening the most important group of β-lactam antibiotics, carbapenems. A plausible solution to overcome the resistance introduced by BLs is the combination of antibiotics and inhibitors. In this thesis efforts are made towards deactivation of a BL, more specifically a carbapenemase, called OXA-48 by the synthesis of inhibitors. The synthetic strategies and computational foundations for a new fragment library are presented within, using four main reactions: Suzuki-Miyaura cross coupling, reductive amination, tetrazole formation and ester hydrolysis. New inhibitors were synthesized and tested towards the activity of OXA-48, the most promising showing IC50 value of 3.3 µM.en_US
dc.identifier.urihttps://hdl.handle.net/10037/22703
dc.language.isoengen_US
dc.publisherUiT Norges arktiske universitetno
dc.publisherUiT The Arctic University of Norwayen
dc.rights.holderCopyright 2020 The Author(s)
dc.rights.urihttps://creativecommons.org/licenses/by-nc-sa/4.0en_US
dc.rightsAttribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)en_US
dc.subject.courseIDKJE-3900
dc.subjectVDP::Matematikk og Naturvitenskap: 400::Kjemi: 440::Organisk kjemi: 441en_US
dc.subjectVDP::Mathematics and natural science: 400::Chemistry: 440::Organic chemistry: 441en_US
dc.titleAntibiotic Resistance Breakers: Design and Synthesis of OXA-48 Inhibitorsen_US
dc.typeMaster thesisen_US
dc.typeMastergradsoppgaveno


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Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)