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Synthesis and structure-activity relationship studies of marine-derived antimicrobial peptides and small cyclic peptidomimetics
(Doctoral thesis; Doktorgradsavhandling, 2023-06-26)Effective antimicrobial drugs are the very core of modern medicine enabling successful prevention and treatment of infectious diseases. However, systemic misuse and overuse of antibiotics in human medicine, as well as in animal husbandry have led to widespread antibiotic-resistance, rendering many of these drugs ineffective. Therefore, there is an urgent need for new treatment options to conventional ... -
Synthesis of 5,7-diarylindoles via Suzuki-Miyaura coupling in water
(Journal article; Tidsskriftartikkel; Peer reviewed, 2021-11-16)The synthesis of novel 5,7-diaryl and diheteroaryl indoles has been explored via efficient double Suzuki–Miyaura coupling. The method notably employs a low catalyst loading of Pd(PPh<sub>3</sub>)<sub>4</sub> (1.5 mol%/coupling) and water as the reaction solvent to obtain 5,7-diarylated indoles without using N-protecting groups in up to 91% yield. The approach is also suitable for N-protected and ... -
Synthesis of 5-,6-, and 7-membered heterocycles from barbituric acid derivatives
(Master thesis; Mastergradsoppgave, 2011-06-10)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 ... -
Synthesis of a novel class of antitubercular peptidomimetics based on β-aminoboronates.
(Doctoral thesis; Doktorgradsavhandling, 2012-11-16)The unique properties of antimicrobial peptides have attracted the attention of chemists since the 1970’s. This class of compounds provides additional tools in the treatment of infections and the work described in this thesis was therefore focused on the synthesis of short peptidomimetics on the basis of modified amino acids and evaluation of their antimicrobial activity. The compounds of choice ... -
Synthesis of a novel tripeptidomimetic scaffold and biological evaluation for CXC chemokine receptor 4 (CXCR4) antagonism
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-05-17)We here report the preparation of a new 2,6,8-trisubstituted bicyclic tripeptidomimetic scaffold through TFA-mediated cyclization of a linear precursor containing three side chains. The introduction of a triphenylmethyl-protected thiol into carboxylic acid containing building blocks through sulfa Michael additions onto α,β-unsaturated hexafluoroisopropyl esters is described. The stereoselectivity ... -
Synthesis of aromatic lactone analogues of Lipoxin A4
(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. -
Synthesis of copper and silver nanoparticles with extracts of berries: A green chemistry approach
(Master thesis; Mastergradsoppgave, 2017-05-15)Nanoparticles are usually defined as particles in a size range of 1-100 nm, and these particles often have different properties than the non-nanoscale material of the same chemical composition. In recent years, as the interest and use of nanoparticles has increased and so has the interest in understanding their behaviour, impact and fate in the environment. In the last decades, there has been special ... -
Synthesis of Indoles and Pyrroles Utilizing Iridium Carbenes Generated from Sulfoxonium Ylides
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-03-20)Metal carbenes can undergo a myriad of synthetic transformations. Sulfur ylides are potential safe precursors of metal carbenes. Herein, we report cascade reactions that involve carbenoids derived from sulfoxonium ylides for the efficient and regioselective synthesis of indoles and pyrroles. The tandem action of iridium and Brønsted acid catalysts enables rapid assembly of the heterocycles from ... -
Synthesis of phorbazoles and breitfussins analogues
(Master thesis; Mastergradsoppgave, 2016-05-18)Breitfussins are a group of a closely related heterocyclic compounds. They consist of a tetracyclic structure with an indole, an oxazole and a pyrrole. The breitfussins exhibit interesting biological activity and analogues synthesis and biological evaluation is ongoing. Phorbazoles have a structural similarity with breitfussins in which a phenol replaces the indole. As a part of this, synthesis of ... -
Synthesis of Potential Metallo-beta-Lactamase Inhibitors
(Master thesis; Mastergradsoppgave, 2011-11-15) -
Synthesis of Potential Metallo-β-Lactamase Inhibitors
(Master thesis; Mastergradsoppgave, 2012-06-04)Oppgaven omhandler syntesen av mulige metallo-beta-lactamaser inhibitorer. -
Synthesis of Sterically Hindered Macrocyclic Ligands via Demetalation of Metallocorroles
(Doctoral thesis; Doktorgradsavhandling, 2016-06-07)Despite important developments in synthetic corrole chemistry, the field has long been handicapped by the lack of procedures for demetalation of metallocorroles. This thesis presents general demetalation methods for metallocorroles. A reductive demetalation method was developed using concentrated H2SO4 with 5-200 equivalent of FeCl2 or SnCl2 as a reducing agent. The method proved to be quite general ... -
Synthesis of substituted (N,C) and (N,C,C) Au(iii) complexes: the influence of sterics and electronics on cyclometalation reactions
(Journal article; Tidsskriftartikkel; Peer reviewed, 2022-03-04)Cyclometalated Au(III) complexes are of interest due to their catalytic, medicinal, and photophysical properties. Herein, we describe the synthesis of derivatives of the type (N,C)Au(OAcF)2 (OAcF = trifluoroacetate) and (N,C,C)AuOAcF by a cyclometalation route, where (N,C) and (N,C,C) are chelating 2-arylpyridine ligands. The scope of the synthesis is explored by substituting the 2-arylpyridine core ... -
Synthesis of thiol-appended gold and rhenium corroles as potential nanoconjugants for gold nanoparticles
(Master thesis; Mastergradsoppgave, 2023-06-10)Photodynamic therapy (PDT) today is an established treatment for a variety of cancers as well as various dermatological conditions, macular degeneration and bacterial and other infections. Treatment involves the administration of a photosensitizer, typically a porphyrin, followed by irradiation with light. The photoexcited sensitizer transfers its excess energy to oxygen in the affected tissue, ... -
Synthesis of XTH inhibitors
(Master thesis; Mastergradsoppgave, 2019-05-15)XTH er en gruppe enzymer som ble oppdaget tidlig på 90 tallet og muligens er involvert i Cuscuta infeksjonen av tomater. En nylig studie gjort ved arktisk og marin biologi UIT viser at Brilliant Blue R250 fungerer som en god inhibitor mot disse enzymene. I dette prosjektet ble det fokusert på å syntetisere strukturelt like molekyler for å potensielt øke vannløseligheten og inhibitoraktiviteten. ... -
Synthesis of β-substituted β-aminoboronates
(Master thesis; Mastergradsoppgave, 2013-05)Recent work at the University of Tromsø has uncovered new α-substituted α- and β-aminoboron containing peptidomimetics that shows antimicrobial, antifungal and antitubercular activity in addition to kinase inhibition and promotion. As a continuation of this work a new approach for the synthesis of β-substituted β-aminoboronates has been developed. The approach involves the non-stereospecific ... -
Synthesis, bioactivity testing, and structure elucidation of antimicrobial peptide analogues derived from Synoicum Turgens
(Mastergradsoppgave; Master thesis, 2023-05-15)A method was developed for synthesizing and isolating two DRPs, with varying levels of success affected by difficulties in the purification process and human error. However, it has shed light on some of the difficulties that may occur and suggestions on how they could be improved. The method developed structure elucidation through sequential reduction and alkylation of the disulfide bridges proved ... -
Synthesis, biological evaluation and molecular modeling of new analogs of the anti-cancer agent 2-methoxyestradiol: potent inhibitors of angiogenesis
(Journal article; Tidsskriftartikkel; Peer reviewed, 2015-03-27)The synthesis, cytotoxicity, inhibition of tubulin polymerization and anti-angiogenic effects of 10 analogs of 2-methoxyestradiol are reported. These efforts revealed that the analog with a 4-pyridine ring in the 17-position, in combination with 2-ethyl- and 3-sulfamate substituents on the steroid A-ring, is the most interesting anti-cancer agent. This compound showed potent inhibitory effects against ... -
Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618
(Journal article; Tidsskriftartikkel; Peer reviewed, 2015-03-05)Abstract: Herein, we describe the synthesis, biological evaluation and molecular docking of the selective PPARb/ d antagonist (4-methyl-2-(4-(trifluoromethyl)phenyl)-N-(2-(5-(trifluoromethyl)-pyridin-2-ylsulfonyl) ethyl)thiazole-5-carboxamide)), CC618. Results from in vitro luciferase reporter gene assays against the three known human PPAR subtypes revealed that CC618 selectively antagonizes ... -
Synthesis, experimental evaluation and molecular modelling of hydroxamate derivatives as zinc metalloproteinase inhibitors
(Journal article; Tidsskriftartikkel; Peer reviewed, 2015-11-28)Enzymes of the M4 family of zinc-metalloproteinases are virulence factors secreted from gram-positive or gram-negative bacteria, and putative drug targets in the treatment of bacterial infections. In order to have a therapeutic value such inhibitors should not interfere with endogenous zinc-metalloproteinases. In the present study we have synthesised a series of hydroxamate derivatives and validated ...