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Showing 1 to 14 of 14 for “"nucleoside analogues"”.
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Synthesis of nucleoside analogues.
A basic introduction to a variety of nucleoside derivatives is described along with a selection of recent syntheses of the said compounds. Initial studies on the synthesis of the key furan based intermediate N-2,5-dihydro-5-(2,2-dimethyl-1,3-dioxolan-4-yl)furanyl trichloroacetamide which when …
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Synthesis of Novel Cyclobutane Nucleoside Analogues
A synthesis of cyclobutane nucleosides is described. The method involved the triflation of a -hydroxymethyl-cyclobutanone and its subsequent displacement by a 6-chloropurinyl anion to generate N-7 and N-9 regioisomers. The stereoselective reduction of the N-alkylated ketones yielded the …
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Application of thermodynamic principles in biocatalytic synthesis of novel nucleoside analogues
Nucleosides and analogues thereof are central molecules in modern cancer therapy and in the fight against viral infections. However, their efficient synthesis is a challenging task for synthetic chemistry. This necessitates lengthy routes and results in low atom economy. Nature’s chemistry set, on …
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Synthesis and Biological Evaluation of Modified Adenosine and Thymidine Nucleoside Analogues
SAMENVATTING In Deel I (Hoofdstuk 1-2) van dit werk beschreven we de synthese van gemodificeerde adenosine en thymidine analogen (zie Figuur 1). Deze verbindingen werden als moleculaire probes gebruikt voor de biologische evaluatie van adenosine-receptoren (ARn, Deel II, Hoofdstuk 3-6), die behoren …
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The Impact of Nucleoside Sugar Modification on Biochemical DNA Transactions
… for the synthesis of oligonucleotides with nucleoside analogues with biased sugar conformations at the 3'-end (growing end) as well as at internucleotide positions. Through a series of thermodynamic, structural and functional studies, we reveal how sugar structure and conformational …
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Mechanism of lipid disorder in HIV infection: apolipoprotein-B kinetics, fat distribution, insulin resistance and adipocytokines in patients taking protease inhibitors or non-nucleoside reverse transcriptase inhibitors
… patients (n=15) and patients taking two nucleoside analogues plus either a protease inhibitor (PI, n=15) or non-nucleoside reverse transcriptase inhibitor (NNRTI, n = 25). The HIV positive treatment groups had mild dyslipidaemia. The apo-B fractional clearance rate (FCR) was reduced in …
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Stereoselective synthesis of artificial C-nucleosides
… and their 2’,3’-didehydro 2’,3’-dideoxy (D4) analogues. We have successfully implemented a divergent synthetic route capable to reach two important, biologically significant groups of compounds. The first two strategic transformations are common for both families of target compounds …
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Structure-aided design of inhibitors of Mycobacterium tuberculosis thimydilate kinase
… relationship by synthesising a series of nucleosides and nucleotides modified at the 2’-, 3’- and 5-positions of the dTMP-scaffold. These analogues were tested for their affinities for TMPKmt. From this, a 2'-chlorine and a 2'-fluorine substituent emerged as the most promising …
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Nucleoside and oligonucleotide approaches towards potential HIV chemotherapies
… which were developed for the synthesis of nucleoside intermediates for oligonucleotide applications were also used to prepare a series of nucleoside analogues derived from uridine, 2'-deoxyuridine and AZT. Crystal structures of six compounds were successfully determined. Anti-HIV activity …
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Adenosine triphosphate is an allosteric inhibitor of coxsackievirus B3 3Dpol
… inhibitors that have been found to date are nucleoside analogues that act directly on the active site, even though global dynamics of the protein that are sensitive to allosteric effects of various mutations have been shown to be important determinants of fidelity. The research presented in …
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Investigating the impact of pharmacological exposures on the developing epigenome
… (AZA) and decitabine (DAC) are both cytidine nucleoside analogues used in the treatment of acute myeloid leukaemia. Following incorporation into DNA, both drugs have been demonstrated to induce depletion of DNA methyltransferases (DNMTs), removal of DNA methylation and induction of DNA damage. …
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Flavonoids and Related Compounds as Nucleoside Transporter Inhibitors
<p>Mammalian nucleoside transporters can be classified into two main categories, namely, equilibrative nucleoside transporters (ENTs) and concentrative nucleoside transporters (CNTs). ENTs are ubiquitous, and mediate sodium-independent bi-directional facilitated diffusion nucleoside transport …
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INVESTIGATION OF ANTIBIOFILM AND ANTIVIRULENCE ACTIVITY OF 5-FLUOROCYTOSINE IN ESCHERICHIA COLI
… strategy. Several antimetabolites and nucleobase/nucleoside analogues, such as 5-fluorocytosine and 5-fluorouracil, have been shown to possess antivirulence activity in Gram negative bacteria like Pseudomonas aeruginosa and Escherichia coli. In my PhD work, based on previous observation that …