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Mastergradsoppgaver i kjemi

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Synthesis of Potential Metallo-beta-Lactamase Inhibitors

Paulsen, Britt (Master thesis; Mastergradsoppgave, 15-Nov-2011)

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URI: http://hdl.handle.net/10037/3821

File(s) in this item: 1

thesis.pdf (5.947Mb)

Protein-protein binding affinities calculated using the LIE method

Andberg, Tor Arne Heim (Master thesis; Mastergradsoppgave, 15-Nov-2011)

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Abstract:	Absolute binding free energies for the third domain of the turkey ovomucoid inhibitor in complex with Streptomyces griseus proteinase B and porcine pancreatic elastase has been calculated using the linear interaction energy method.
URI:	http://hdl.handle.net/10037/3820

File(s) in this item: 1

thesis.pdf (2.515Mb)

Demetalation of metallocorroles

Capar, Can (Master thesis; Mastergradsoppgave, Oct-2008)

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Abstract:

Although the chemistry of corroles has grown spectacularly in recent years, the field has been marred by the lack of convenient protocols for demetalation of metallocorroles. In this thesis, I have developed a superior procedure for demetalating copper corroles with concentrated H2SO4 and 5-200 equiv FeCl2 or SnCl2. The yields obtained with this reductive procedure are generally substantially better than with HCl3/H2SO4, CH2Cl2/H2SO4, or H2SO4 alone. With an oxidation-prone metallocorrole such as Cu[T(p-OMeP)C], the reductive protocol was essential for obtaining any measurable yield of the free base at all. Free-base β-octabromo-mesotriarylcorroles were also obtained in pure form, in good yields, and with relative ease via this procedure.

URI:

http://hdl.handle.net/10037/3809

File(s) in this item: 1

thesis.pdf (1.468Mb)

Purification and characterization of a salt tolerant metallo-beta-lactamase from Aliivibrio salmonicida

Kristiansen, Anders (Master thesis; Mastergradsoppgave, Jul-2011)

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Abstract:

Beta-lactamases are enzymes that inactivate beta-lactam antibiotics by hydrolyzing the amide bond that exists in the beta-lactam ring, disrupting the ring structure and make the antibiotics nonfunctional against bacteria. Metallo-beta-lactamases (MBLs) are a group of beta-lactamases which needs metal ions bound to its active site in order to function and are an important factor in many bacteria in order to be resistant to antibiotics. Resistance to antibiotics is a serious health problem which increases with excessive use of antibiotics. This study is based on the purification and characterization of MBL from the psychrophilic organism Aliivibrio salmonicida which is the causative agent for the Hitra disease, or cold-water vibrosis, in seawater-farmed Atlantic salmon (Salmo salar). Characterization of asMBL has revealed interesting properties in regards of temperature-, salt-, pH optimum and enzyme kinetics. asMBL properties have been compared to VIM-7, a MBL isolated from hospital which thrives in mesophilic conditions. Compared to VIM-7, asMBL proves to be adapted to the colder and saltier environment of the seawater. asMBL enzyme kinetics have also been compared to MBLs from human pathogenic bacteria and asMBL showed a general lower enzymatic efficiency in terms of lower kcat and higher Km at the same experimental conditions as the other MBLs. Nitrocefin, the substrate used for the characterization of asMBL, had its stability in temperature, pH and Tris investigated. From these investigations it seems plausible that nitrocefin is auto-hydrolyzed in a synergetic matter when present at high pH and in Tris buffer. An attempt to crystallize the protein and retrieve a structure was unsuccessful as it turns out that the protein seems to be aggregating at high concentrations.

URI:

http://hdl.handle.net/10037/3684

File(s) in this item: 1

thesis.pdf (5.496Mb)

Synthesis of 5-,6-, and 7-membered heterocycles from barbituric acid derivatives

Guyader, David (Master thesis; Mastergradsoppgave, 10-Jun-2011)

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Abstract:

SUMMARY A new procedure has been developed for the synthesis of barbituric acid derivatives. The reactions were performed under solvent free conditions without any catalyst. Employing this synthetic route, a large number of chalconoids and 5-,6-, and 7-membered heterocycles have been successfully synthesized in a very short time. The chalconoids have been synthesized from a barbituric derivative and substituted benzaldehydes. The effect of different substituents on the yield of the reaction has been observed. This study revealed that electron-donating groups were more efficient in general than electron-withdrawing groups as substituents. The position of the substituents at the benzene ring of the chalconoids also seems to affect the yield of this reaction. Using experimental design optimize the reactions in a significant manner. 5-, 6-, and 7-membered heterocycles have been produced by reacting the chalconoids and a range of dinucleophiles. Structure of some of the derivatives have been obtained by X-ray analysis and complete the spectroscopic investigations. Biological activity of some compounds has been highlighted from kinase testing.

URI:

http://hdl.handle.net/10037/3683

File(s) in this item: 1

thesis.pdf (7.498Mb)

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Mastergradsoppgaver i kjemi

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Mastergradsoppgaver i kjemi

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