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1

Collins, James P. "Prebiotic Synthesis of Pyrimidine Nucleosides." Thesis, Georgia Institute of Technology, 2005. http://hdl.handle.net/1853/14095.

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The problem of forming a glycosidic bond between ribose and the free nucleoside bases to produce beta-nucleosides under plausible prebiotic conditions is commonly referred to in origin of life research as The Nucleoside Problem. The lack of a general solution to this problem currently represents one of the largest stumbling blocks to the RNA world hypothesis and many other theories regarding the origin of life. Over thirty years ago the purine nucleosides were successfully synthesized by drying the fully-formed bases and ribose together in the presence of divalent metal ion salts. However, gly
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2

Xu, Kuiying. "Pyrrolo[2,3-d]pyrimidine, Pyrazolo[3,4-d]pyrimidine and Triazolo[4,5-d]pyrimidine nucleosides and oligonucleotides: Synthesis, physical properties and base-pairing = Pyrrolo[2,3-d]pyrimidin, Pyrazolo[3,4-d]pyrimidin und Triazolo[4,5-d]pyrimidin nucleoside und oligonucleotide: Synthese, physikalische Eigenschaften und Basenpaarung /." Osnabrück, 2008. http://opac.nebis.ch/cgi-bin/showAbstract.pl?sys=000254557.

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3

Hill, Matthew D. (Matthew Dennis). "Direct synthesis of pyridine and pyrimidine derivatives." Thesis, Massachusetts Institute of Technology, 2008. http://hdl.handle.net/1721.1/43776.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 2008.<br>Vita.<br>Includes bibliographical references.<br>I. Synthesis of Substituted Pyridine Derivatives via the Ruthenium-Catalyzed Cycloisomerization of 3-Azadienynes. The two-step conversion of various N-vinyl and N-aryl amides to the corresponding substituted pyridines and quinolines, respectively, is described. The process involves the direct conversion of amides, including sensitive N-vinyl amides, to the corresponding trimethylsilyl alkynyl imines followed by a ruthenium-catalyzed protodesilylation and cyclois
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4

Chan, Heng Ming. "Synthesis of pyrimidine C-nucleoside analogues and triphosphate derivatives." Thesis, Boston College, 2008. http://hdl.handle.net/2345/36.

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Five pyrimidine C-nucleosides were prepared via Heck-type coupling reactions. These derivatives are designed to mimic dC and dU (or T). The minor groove O2 carbonyl in each derivative is replaced by a hydrogen, a fluorine, or a methyl group. The hydrogen-substituted dC analogue was converted into a 2’,3’-dideoxynucleoside, which was converted into a 5’-triphosphate derivative. The other two dC analogues were transformed into 5’-triphosphate derivatives immediately after Heck coupling reactions. These analogues will allow an examination of the nature and role of minor groove interactions betwee
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5

Sullivan, Shannon M. "Synthesis of 2,4-disubstituted pyrimidine derivatives as potential 5-HT7 receptor antagonist." unrestricted, 2008. http://etd.gsu.edu/theses/available/etd-05052008-153400/.

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Thesis (M.S.)--Georgia State University, 2008.<br>Title from file title page. Lucjan Strekowski, committee chair; A.L. Baumstark, Gabor Patonay, Doyle Barrow , committee members. Electronic text (68 p. : ill.) : digital, PDF file. Description based on contents viewed June 23, 2008. Includes bibliographical references (p. 42-430.
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6

蘇雅頌 and Ngar-chung Nellie So. "Pyrimidine nucleotide biosynthesis in adult angiostrongylus Cantonensis (Nematoda : Metastrongyloidea)." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 1993. http://hub.hku.hk/bib/B3123320X.

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7

Taleli, Lebusetsa. "Radiosynthesis of various pyrimidine derivatives and determining their uptake into cells." Thesis, Cape Peninsula University of Technology, 2009. http://hdl.handle.net/20.500.11838/744.

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Thesis (MTech (Chemistry))--Cape Peninsula University of Technology, 2009<br>N3-substituted pyrimidine nucleoside derivatives containing either an iodovinyl moiety or an allyl group, i.e. [121]-N3-(3-iodoprop-2-en- l -yl)thymidine, (1~-711 and e21]-N3-(prop-2-enl- yl)-5-iodo-Z'-deoxyuridine, (1~_10, were synthesised and preliminarily evaluated by determining their uptake into CHO-Kl cells. Compound e~-711 was designed to be a delivery vector of 121: into the DNA of the cells, while (1~_10 was designed to serve as a control. Compound (1231]-711 was also intended to have a higher metabolic
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8

McFadden, Helen Georgina, and n/a. "Synthesis and herbicidal properties of some pyrazole and pyrimidine heteocycles." University of Canberra. Biomedical Sciences, 1992. http://erl.canberra.edu.au./public/adt-AUC20060918.160845.

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Four main series of novel heterocyclic compounds were successfully syniliesised. Two of these series were found to be post-emergence herbicides with the activities of each being based on a different mode of action. The (pyrazole-4-yl)alkanones are inhibitors of protoporphyrinogen oxidase, an enzyme in chlorophyll biosynthesis, whereas alkyl 3-arylsulfonylamino- 3-methyllhio-2-(pyrimidin-2-ylcarbamoyl)acrylates and pyrimidin-2-yl 3-(2- chlorophenyl)sulfonyl-amino-3-methylthio-2-cyanoacrylamides (collectively termed "vinylogous sulfonylureas") are inhibitors of acetohydroxy acid synthase (AHAS).
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9

Sūdžius, Jurgis. "Synthesis And Properties Of Pyrimidine Derivatives – Potent Carbonic Anhydrase Inhibitors." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2011. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2011~D_20110519_082332-05105.

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The aim of the work was design of pyrimidine derivatives – potent carbonic anhydrase (CA) inhibitors. Theoretical investigation of interaction of 4-[N-(pyrimidin-4-yl)]aminobenzenesulfonamides containing substituents at 2-, 5- and 6- positions of pyrimidine ring with an active site of hCAs suggested that these compounds can fit into an active site of the enzymes and should interact with them as typical hCA inhibitors. Synthesis of target compounds was carried out by substitution of chloro group at 4,6-dichloropyrimidines containing cyano-, formyl- or nitro groups at position 5 of the pyrimidin
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10

Buntain, I. G. "The design, synthesis and testing of inhibitors of pyrimidine biosynthesis." Thesis, University of Strathclyde, 1985. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.372118.

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11

Barnes, Samuel. "Synthesis of 2,4-Disubstituted Pyrimidines of Possible Biological Interest." Digital Archive @ GSU, 2008. http://digitalarchive.gsu.edu/chemistry_theses/10.

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The synthesis of 2,4-disubstituted pyrimidine derivatives is described. The synthetic route involved the addition reaction of lithiated intermediates, mostly heterocycles, to position 4 of 2-chloropyrimidine to give a dihydropyrimidine intermediate which was oxidized back to a pyrimidine. This was followed by nucleophilic aromatic substitution with various amines of the chlorine in the position 2. A number of compounds were prepared which showed binding towards various serotonin receptors in preliminary biological evaluation.
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12

Liang, Yong. "Novel Approaches for the Synthesis of C-5 Modified Pyrimidine Nucleosides." FIU Digital Commons, 2014. http://digitalcommons.fiu.edu/etd/1591.

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The antiviral or anticancer activities of C-5 modified pyrimidine nucleoside analogues validate the need for the development of their syntheses. In the first half of this dissertation, I explore the Pd-catalyzed cross-coupling reaction of allylphenylgermanes with aryl halides in the presence of SbF5/TBAF to give various biaryls by transferring multiple phenyl groups, which has also been applied to the 5-halo pyrimidine nucleosides for the synthesis of 5-aryl derivatives. To avoid the use of organometallic reagents, I developed Pd-catalyzed direct arylation of 5-halo pyrimidine nucleosides. It
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13

McDonald, Robert Andrew. "Synthesis and characterization of chiral liquid crystals incorporating pyrimidine/thiophene moieties." Thesis, University of Hull, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.445723.

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14

Simkovsky, Nadja Melitta. "Synthesis of some potential IKK inhibitors based around a pyrimidine scaffold." Thesis, University of Liverpool, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.367619.

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15

Pretorius, Izak Stefanus. "Synthesis, characterisation and antimalarial activity of quinoline–pyrimidine hybrids / Izak Stefanus Pretorius." Thesis, North-West University, 2012. http://hdl.handle.net/10394/8105.

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The world suffers under the immense threat of malaria with about 1 million people dying and a further 500 million people getting infected and debilitated by the disease each year. It has a negative effect on the economic growth in developing countries that already battles with political unrest, civil wars, famine and the effect of diseases like tuberculosis and HIV/AIDS. Resistance against the first line drugs such as the quinolines and the antifolate combination drugs makes the fight against malaria increasingly difficult and has prompted studies into alternative chemotherapeutic treatments o
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16

Parsons, Rachel. "The design and synthesis of pyrimidine based cyclin-dependent kinase (CDK) inhibitors." Thesis, University of Newcastle Upon Tyne, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.408491.

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17

Juškėnas, Robertas. "Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2014. http://vddb.library.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576.

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The development of heterocyclic chemistry is important for various science areas and for the industry. The main task of this branch of chemistry is the search for the new, more effective synthetic methods for obtaining heterocyclic derivatives. That covers not only the formation of heterocycles, but also their functionalization, which leads to the creation of compounds having various chemical and physical properties. The accomplishments of this area are applied in biochemistry, pharmacochemistry, photophysics and other branches of science and industry. The creation of effective heterocycles sy
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18

Bean, Heather D. "Prebiotic synthesis of nucleic acids." Diss., Atlanta, Ga. : Georgia Institute of Technology, 2008. http://hdl.handle.net/1853/28259.

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Thesis (M. S.)--Chemistry and Biochemistry, Georgia Institute of Technology, 2008.<br>Committee Chair: Hud, Nicholas V.; Committee Member: Fox, Ronald F.; Committee Member: Lynn, David G.; Committee Member: Powers, James C.; Committee Member: Wartell, Roger M.; Committee Member: Williams, Loren D.
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19

Walji, Dhiran. "A radical approach towards the synthesis of novel pyridine and pyrimidine based heterocycles." Thesis, Available from the University of Aberdeen Library and Historic Collections Digital Resources, 2009. http://digitool.abdn.ac.uk:80/webclient/DeliveryManager?application=DIGITOOL-3&owner=resourcediscovery&custom_att_2=simple_viewer&pid=62164.

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20

Howie, Colin. "The design, synthesis and testing of hydantoin derivatives as inhibitors of pyrimidine biosynthesis." Thesis, University of Glasgow, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.278514.

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21

LAMBERTUCCI, Catia. "Synthesis, Characterization, and Biological Activity of Purine and Pyrimidine Nucleoside and Nucleotide Analogues." Doctoral thesis, Università degli Studi di Camerino, 2008. http://hdl.handle.net/11581/401762.

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Purine and pyrimidine nucleosides and nucleotides are constituents of fundamental structures of the cells. In fact, they are constituents of nucleic acids and their structure is present in several coenzymes involved in cellular reduction/oxidation processes, like nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD). Furthermore ATP is the source of energy that drive the cellular metabolic reactions. 3'-5'-cyclicadenosinemonophosphate (cAMP) acts as second messenger controlling the activation of metabolic pathways. The biological relevance of these molecules is also due
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22

Rayala, Ramanjaneyulu. "Design and Synthesis of Novel Nucleoside Analogues: Oxidative and Reductive Approaches toward Synthesis of 2'-Fluoro Pyrimidine Nucleosides." FIU Digital Commons, 2015. http://digitalcommons.fiu.edu/etd/2172.

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Fluorinated nucleosides, especially the analogues with fluorine atom(s) in the ribose ring, have been known to exert potent biological activities. The first part of this dissertation was aimed at developing oxidative desulfurization-fluorination and reductive desulfonylation-fluorination methodologies toward the synthesis of 2'-mono and/or 2',2'-difluoro pyrimidine nucleosides from the corresponding 2'-arylthiopyrimidine precursors. Novel oxidative desulfurization-difluorination methodology was developed for the synthesis of α,α-difluorinted esters from the corresponding α-arylthio esters, whe
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23

Sakthivel, K. "Studies on the synthesis of new aminonucleosides: reactions of sulphonylated pyrimidine necleosides with amines." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 1996. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2840.

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24

Lebar, Matthew D. "Antarctic Tunicates and Endophytic Fungi: Chemical Investigation and Synthesis." Scholar Commons, 2010. http://scholarcommons.usf.edu/etd/3638.

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Drug discovery is reliant on new developments in natural product chemistry as well as advances in chemical synthesis. The interconnectivity and interdependence of natural and synthetic investigation in drug discovery is evident. The chemical exploration reported herein elaborates the relationship between natural product chemistry and chemical synthesis. Of particular interest are chemicals from organisms residing in less accessible environments, particularly Antarctica and endophytic microbial communities. Degradation via reductive ozonolysis of palmerolide A, a macrocyclic polyketide isolated
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25

Niazy, Abdurahman. "Investigating the Ability of Pseudomonas aeruginosa pyrE Mutants to Grow and Produce Virulence Factors." Thesis, University of North Texas, 2014. https://digital.library.unt.edu/ark:/67531/metadc700016/.

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Pseudomonas aeruginosa are medically important bacteria that are notorious for causing nosocomial infections. To gain more knowledge into understanding how this organism operates, it was decided to explore the pyrimidine biosynthetic pathway. Pyrimidine synthesis, being one half of the DNA structure, makes it a very important pathway to the organism’s survivability. With previous studies being done on various genes in the pathway, pyrE has not been studied to the fullest extent. To study the function of pyrE, a site directed mutagenesis was done to completely knock out pyrE, which encodes the
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26

GIACCHELLO, ILARIA. "Synthesis of properly substituted pyridine and pyrimidine derivatives and their biological evaluation as potential antiviral agents." Doctoral thesis, Università degli studi di Genova, 2019. http://hdl.handle.net/11567/940944.

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Influenza A viruses (IAVs) belong to the Orthomixoviridae, a family of enveloped viruses with a single-stranded negative-sense and eight-segmented RNA genome. They are the most prevalent pathogens for both humans and animals, causing the so-called seasonal flu and widespread pandemics. A part from the use of vaccines, viral infections can be inhibited at several crucial steps by the use of antiviral agents. It is possible to have an antiviral effect both targeting important proteins for the virus life cycle and targeting host proteins that play crucial roles during influenza virus infection. R
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27

Nikmal, Arif. "Studies towards a chemical origins of RNA : divergent prebiotic synthesis of pyrimidine and 8-oxo-purines ribonucleotides." Thesis, University College London (University of London), 2018. http://discovery.ucl.ac.uk/10046328/.

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Elucidating a prebiotic plausible nucleotide synthesis is considered one of the greatest challenges in the origins of life research. Although separate synthesis that account for the pyrimidine and purine ribonucleotides have been developed, no divergent synthesis from a single precursor has yet been developed that accounts for the synthesis of both pyrimidine and purine ribonucleotides. Furthermore, the reported prebiotic synthesis of pyrimidine and purine nucleotides are not mutually compatible and could not co-operate under similar conditions. This thesis proposes a divergent synthesis of bo
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28

Bera, S. "Functionalisation of the carbohydrate moieties of pyrimidine nucleosides: synthesis of amino and sulphur modified thymidines and uridines." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 1996. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/3033.

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29

GRECO, CHIARA. "Synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine derivatives active as SGK1, Fyn and Src kinases inhibitors." Doctoral thesis, Università degli studi di Genova, 2020. http://hdl.handle.net/11567/1001600.

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The pathogenesis of many cancers is characterized by mutations, overexpression and dysregulation of protein kinases. As a result, increasing attention has been directed towards the identification of novel kinase inhibitors for cancer therapy. The work performed here focuses on the synthesis of a series of pyrazolo[3,4-d]pyrimidine derivatives as inhibitors of the serine-threonine kinase SGK1, and the tyrosine kinases Fyn and Src. The first set of compounds are analogues of the in house SGK1 inhibitor SI113 which had previously demonstrated anti-cancer activity. In fact SI113 resulted to b
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30

Berthod, Thomas. "Synthèse d'oligonucléotides comportant des lésions radio- et photo-induites des bases pyrimidiques." Université Joseph Fourier (Grenoble ; 1971-2015), 1996. http://www.theses.fr/1996GRE10224.

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De nombreuses modifications des bases de l'adn peuvent etre generees par divers facteurs comme les agents oxydants ou cancerigenes, les rayonnements afin d'evaluer les consequences biologiques et physico-chimiques de ces dommages, il est necessaire de posseder des modeles plus complexes de ceux-ci qui peuvent etre obtenus par leur incorporation dans des oligonucleotides par voie chimique. Ce travail est consacre a la preparation de fragments d'adn contenant des derives de la 2'-desoxyuridine. Le premier volet de ce travail a consiste a preparer un synthon phosphoramidite de la 5-formyl-2'-deso
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31

Raux, Elizabeth A. "Synthesis of Selective 5-HT6 and 5-HT7 Receptor Antagonists." Digital Archive @ GSU, 2010. http://digitalarchive.gsu.edu/chemistry_theses/32.

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The development of novel selective 5-HT6 and 5-HT7 receptor antagonists is an ever-growing area of interest among medicinal chemists. The potential of developing a therapeutic agent useful as an antipsychotic or antidepressant, as well as the possibility to develop a drug for Alzheimer’s disease and obesity has led to an increase in synthesis of possible lead compounds. The synthesis of unfused biheteroaryl derivatives is described within. The derivatives have been evaluated for binding affinity at 5-HT2A, 5-HT6 and 5-HT7 receptors. The most potent 5-HT6 receptor antagonists include a benzene
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32

REDENTI, SARA. "DESIGN, SYNTHESIS AND CHARACTERIZATION OF GSK-3β AND CK-1δ INHIBITORS". Doctoral thesis, Università degli Studi di Trieste, 2017. http://hdl.handle.net/11368/2908172.

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Glycogen Synthase Kinase 3-β (GSK-3β) and Casein Kinase 1-δ (CK-1δ) are both highly conserved serine/threonine protein kinases that seem to be involved in neuroinflammation and in the development and progression of several disorders of the central nervous system (CNS), such as Alzheimer’s disease (AD) and Parkinson’s disease (PD). In particular, both are related to the hyperphosphorylation of tau-protein, one of the major hallmark of AD and other taupathies. So, the inhibition of GSK-3β and or CK-1δ could represent a strategy for the treatment of these unmet diseases. The main purpose of this
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33

Klenc, Jeffrey D. "Design and Synthesis of Novel Serotonin Receptor Ligands." Digital Archive @ GSU, 2010. http://digitalarchive.gsu.edu/chemistry_diss/50.

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Novel and potent ligands to the serotonin7 (5-HT7) receptor have been synthesized. The synthesized compounds include a set of substituted pyrimidines which show high affinity to the 5-HT7 receptor, synthesized by previously described methods [1,2] in high yield. Comparing the affinities of substituted pyrimidines to previously calculated models [3,4] yielded new hypotheses about the nature of interaction between the pyrimidine ligands and the 5-HT7 binding site. Several new series of compounds were synthesized by various methods to validate these hypotheses, including a conjugate addition t
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34

Barbosa, Sara Isabel Cadinha. "Compostos que interferem no metabolismo dos purina- e pirimidina-nucleótidos: utilização como agentes terapêuticos." Master's thesis, [s.n.], 2015. http://hdl.handle.net/10284/5160.

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Projeto de Pós-Graduação/Dissertação apresentado à Universidade Fernando Pessoa como parte dos requisitos para obtenção do grau de Mestre em Ciências Farmacêuticas<br>O conteúdo deste trabalho será desenvolvido em dois temas principais, um referente à utilização de compostos que interferem no metabolismo dos purina- e pirimidinanucleótidos como agentes antineoplásicos e outro referente à sua utilização como agentes antivirais. A síntese dos nucleótidos envolve a construção de ácidos nucleicos e a inserção dos derivados de nucleótidos noutras vias bioquímicas, sendo responsável por inúmera
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35

Le, Hir de Fallois Loic. "Synthèse et étude de nucléosides et nucléotides inhibiteurs de la ribonucléotide réductase." Université Joseph Fourier (Grenoble), 1995. http://www.theses.fr/1995GRE10158.

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La ribonucleotide reductase (rnr) est l'enzyme qui catalyse la reduction des ribonucleotides en desoxyribonucleotides. En raison de son role fondamental dans la synthese de l'adn, cette enzyme est une cible cle de la recherche de nouveaux agents antitumoraux. Dans le but d'inhiber cette enzyme nous avons synthetise des analogues de substrats. Nous avons synthetise et etudie les proprietes des premiers nucleosides thionitrites, les 2'-desoxy-2'-s-nitroso-uridine et -cytidine. Nous avons demontre que ces thionitrites liberent du monoxyde d'azote (no) qui est un inhibiteur de la ribonucleotide re
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36

Mederic, Christine. "Amplification du dna ribosomal nucleolaire chez l'euclene carencee en vitamine b::(12) : role possible de cette vitamine dans la synthese terminale des acides nucleiques." Paris 7, 1988. http://www.theses.fr/1988PA077116.

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37

Lee, Jeong-Hwan. "Synthesis of pyrrolo[2,3-d]pyrimidines and pyrazino[2,3-d]pyrimidines and their biological activities." Thesis, University of Strathclyde, 2010. http://oleg.lib.strath.ac.uk:80/R/?func=dbin-jump-full&object_id=14350.

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38

Barnes, Samuel. "Synthesis of 2, 4-distributed pyrimidines of possible biological interest." unrestricted, 2008. http://etd.gsu.edu/theses/available/etd-05012008-164917/.

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Thesis (M.S.)--Georgia State University, 2008.<br>Title from file title page. Lucjan Strekowski, committee chair; A.L. Baumstark, Jerry Smith, committee members. Electronic text (83 p. : ill.) : digital, PDF file. Description based on contents viewed August 8, 2008. Includes bibliographical references (p. 44-46).
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39

Tkacz, Victoria. "Synthesis of thieno[2,3]-pyrimidines as candidate antileishmanial agents." Connect to resource, 2006. http://hdl.handle.net/1811/6636.

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Thesis (Honors)--Ohio State University, 2006.<br>Title from first page of PDF file. Document formatted into pages: contains 14 p.; also includes graphics. Includes bibliographical references (p. 8). Available online via Ohio State University's Knowledge Bank.
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40

Do, Khoa Quang. "Design, Synthesis and Binding Studies of Trisubstitutedpyrazolo[3,4-d]pyrimidines." Thesis, Griffith University, 2006. http://hdl.handle.net/10072/367533.

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Pyrazolo[3,4-d]pyrimidines were known as adenosine antagonists at the rat A1 and A2A adenosine receptors based on our previous studies. In this study, 245 pyrazolo[3,4-d]pyrimidines derivatives with various benzyl substitutents at N-1 and various hydrophobic side chains at C-4 and C-6 were synthesized and screened at the human A1, A2A and A3 adenosine receptors. 14 out of 245 compounds were resynthesized and purified to determine the Ki values of these compounds at the human A1 adenosine receptor. Chapter 1 of the thesis is a literature review of adenosine research. It describes the physiology
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41

Spencer, Keith. "Parallel synthesis of C-nucleosides." Thesis, University of Oxford, 1999. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.325958.

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42

McIntyre, Neil A. "Synthesis of ring-constrained thiazolylpyrimidines : inhibitors of cyclin-dependent kinases /." St Andrews, 2007. http://hdl.handle.net/10023/353.

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43

Doveston, Richard Gerard. "Oxepine-pyrimidinone natural products : the total synthesis of (±)-janoxepin." Thesis, University of York, 2012. http://etheses.whiterose.ac.uk/2397/.

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The first total synthesis of (±)-janoxepin I, an antiplasmodial oxepine-pyrimidinone natural product isolated from the fungus Aspergillus janus is described herein. Chapter 1 provides an introduction to janoxepin I and related natural products that have been reported in the literature. In Chapter 2, the available methods for the synthesis of oxepines and pyrimidinones are reviewed, before the preparation of dihydro-oxepine VI from readily available starting materials II-V is described. The enamine side-chain seen in janoxepin I was introduced by way of aldol-addition to the ketopiperazine ring
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44

Ahmad, Omar K. (Omar Khaled). "Stereoselective monoalkyl diazene synthesis for mild reductive transformations : direct synthesis of densely substituted pyridines and pyrimidines." Thesis, Massachusetts Institute of Technology, 2011. http://hdl.handle.net/1721.1/62722.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 2011.<br>Vita. Cataloged from PDF version of thesis.<br>Includes bibliographical references.<br>I. N-Isopropylidene-N'-2-Nitrobenzenesulfonyl Hydrazine. A Reagent for Reduction of Alcohols via the Corresponding Monoalkyl Diazenes The development of a new reagent N-isopropylidene-N'-2-nitrobenzenesulfonyl hydrazine (IPNBSH) is described. IPNBSH is used in the reduction of alcohols via the loss of dinitrogen from transiently formed monoalkyl diazene intermediates that can be accessed by sequential Mitsunobu displacement,
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45

Vieira, Andreia Sofia da Costa. "Rethinking Triazoles as Antifungals: Synthesis and Evaluation of New Triazole Derivatives." Master's thesis, Universidade Nova de Lisboa, Instituto de Tecnologia Química e Biológica António Xavier, 2017. http://hdl.handle.net/10362/81407.

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"In the last decades, fungal infections have become a serious problem, mainly due to the excessive use of this reduced number of drugs, leading to an increase of acquired resistances1. Therefore, it is urgent to develop new and more effective antifungal medicines. The main objective of this master's thesis was the development of novel antifungal drugs, based on triazoles and pyrimidines, combining two groups with antifungal properties, known to be active in combinatorial therapies, in a single molecule. For the synthesis of these compounds, Huisgen's 1,3-dipolar cycloaddition methodologies, c
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46

Felkel, Michael [Verfasser]. "Synthese Pyrimidin-basierter 24-Desoxybiphenomycin B-Analoga / Michael Felkel." München : Verlag Dr. Hut, 2011. http://d-nb.info/1018983074/34.

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47

Poulsen, Sally-Ann, and n/a. "Pyrazolo(3,4-d)pyrimidines: Synthesis and Structure-Activity Relationships for Binding to Adenosine Receptors." Griffith University. School of Science, 1996. http://www4.gu.edu.au:8080/adt-root/public/adt-QGU20050901.161632.

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Chapter 1 of thesis is a literature review of adenosine research. The central importance of the contributions of both classical pharmacology and, more recently, molecular biology to adenosine research is demonstrated. These disciplines have enabled the classification and characterisation of adenosine receptors and as well an understanding of the physiological significance of endogenous adenosine. The significant benefits of developing therapeutics for regulation of the diverse physiological functions of adenosine, by regulation of adenosine receptors, is outlined. For this therapeutic potentia
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48

Poulsen, Sally-Ann. "Pyrazolo(3,4-d)pyrimidines: Synthesis and Structure-Activity Relationships for Binding to Adenosine Receptors." Thesis, Griffith University, 1996. http://hdl.handle.net/10072/365893.

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Chapter 1 of thesis is a literature review of adenosine research. The central importance of the contributions of both classical pharmacology and, more recently, molecular biology to adenosine research is demonstrated. These disciplines have enabled the classification and characterisation of adenosine receptors and as well an understanding of the physiological significance of endogenous adenosine. The significant benefits of developing therapeutics for regulation of the diverse physiological functions of adenosine, by regulation of adenosine receptors, is outlined. For this therapeutic potentia
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49

Blake, Ava L. "Synthesis of Substituted Pyrimidines and Pyridines as Ligands to the 5-HT7 Receptor." Digital Archive @ GSU, 2010. http://digitalarchive.gsu.edu/chemistry_theses/29.

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Of the seven existing classes of serotonin receptors, the 5-HT7 receptors (5-HT7Rs) are the most recently discovered. Abundance of 5-HT7 in the central nervous system is suggestive of the receptor’s role in several physiological and pathophysiological functions. Existing research has afforded a number of compounds exhibiting specific affinity to the receptor. These selective ligands can provide structural information about the receptor and can serve as the foundation for pharmacological profiling . This thesis describes the synthesis of substituted pyrimidines and pyridines for affinity to the
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McLachlan, Janice. "Synthesis of 2-amino-4-(thiazol-5-yl) pyrimidines as potential kinase inhibitors." Thesis, University of Edinburgh, 2006. http://hdl.handle.net/1842/12637.

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