Дисертації з теми "Macroline"
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Pett, Richard. "Total synthesis of the macroline-related alkaloid (±)-alstonerine." Thesis, Imperial College London, 2013. http://hdl.handle.net/10044/1/17842.
Повний текст джерелаGaret, Florence. "Mode d'action des antibiotiques du groupe des macrolides." Paris 5, 1988. http://www.theses.fr/1988PA05P265.
Повний текст джерелаTalbi, Patrice. "Macrolides et éradication de Hélicobacter pylori." Bordeaux 2, 1994. http://www.theses.fr/1994BOR23066.
Повний текст джерелаZarate, Ruiz Griselda Araceli. "Vers la synthèse totale de la Thuggacine A." Thesis, Montpellier, Ecole nationale supérieure de chimie, 2011. http://www.theses.fr/2011ENCM0002.
Повний текст джерелаThe herein presented study is concerned by the synthesis of the C12-C25 fragment of Thuggacine A, a potent antibiotic macrolide, through two distinct synthetic pathways. The first synthetic pathway enabled us to form 4 among 5 stereogenic centers from (R)-glyceraldehyde acetonide. The key induction asymmetric step showed that the 3 chiral centers C18-C20 were formed with a syn-configuration as in Thuggacine A and the C17-C18 stereocenters were anti-configurated, a result confirmed by X-ray cristallography of compound 84. Low yields and low diastereocontrol of these four chiral centers led us to envisage an alternative synthetic strategy. The second synthetic pathway enabled us ti obtain the C13-C25 fragment within ten linear steps and a high diastereocontrol of the five required stereogenic centers. The 4 chiral centers C-17 to C-20 were formed through two Evans's aldolization steps while the stereochemistry of the C16 center was secured by an allenyl-stannane homologation
Vicarini, Hubert. "Résistance inductible et constitutive des streptocoques et des entérocoques à l'érythromycine." Paris 5, 1997. http://www.theses.fr/1997PA05P007.
Повний текст джерелаPeyramaure, Elisabeth. "Distribution de trois classes d'antibiotiques dans l'organisme : les macrolides, les quinolones et les céphalosporines." Paris 5, 1991. http://www.theses.fr/1991PA05P193.
Повний текст джерелаJensen-Cain, Donna Marie. "Macrolide Resistance in Mycobacterium avium." Diss., Virginia Tech, 1997. http://hdl.handle.net/10919/30560.
Повний текст джерелаPh. D.
Cousin, Sydney Louis. "Macrolide resistance in Neisseria gonorrhoeae /." Thesis, Connect to this title online; UW restricted, 2003. http://hdl.handle.net/1773/5078.
Повний текст джерелаBassuel, Virginie. "Macrolides, streptogramines et staphylocoques : étude d'une nouvelle résistance à l'érythromycine par efflux et d'une nouvelle streptogramine, injectable, le RP 59500." Paris 5, 1993. http://www.theses.fr/1993PA05P210.
Повний текст джерелаLovmar, Martin. "Macrolide Antibiotics in Bacterial Protein Synthesis." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis : Univ.-bibl. [distributör], 2005. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-6009.
Повний текст джерелаLee, Hoyoung. "Evolution of macrolide antibiotics in E.coli /." May be available electronically:, 2008. http://proquest.umi.com/login?COPT=REJTPTU1MTUmSU5UPTAmVkVSPTI=&clientId=12498.
Повний текст джерелаShang, Shiying. "A unified synthetic approach to polyketides having both skeletal and stereochemical diversity /." Access full-text from WCMC, 2008. http://proquest.umi.com/pqdweb?did=1528359411&sid=7&Fmt=2&clientId=8424&RQT=309&VName=PQD.
Повний текст джерелаHu, Thomas Qiuxiong. "Synthesis and conformational studies of 10, 10-dimethyltridecanolide." Thesis, University of British Columbia, 1988. http://hdl.handle.net/2429/27960.
Повний текст джерелаScience, Faculty of
Chemistry, Department of
Graduate
Rey, Allan W. "Synthetic studies directed towards the antineoplastic macrolide bryostatins." Thesis, University of Ottawa (Canada), 1990. http://hdl.handle.net/10393/5938.
Повний текст джерелаJones, Tracey Ann. "Macrolide antibiotic resistance and production in Streptomyces narbonensis." Thesis, University of Leicester, 1997. http://hdl.handle.net/2381/29668.
Повний текст джерелаChin, Alex C. "Anti-inflammatory effects of the macrolide antibiotic tilmicosin." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1998. http://www.collectionscanada.ca/obj/s4/f2/dsk2/ftp03/MQ31336.pdf.
Повний текст джерелаO'Hagan, D. "Biosynthesis studies on the polyether and macrolide antibiotics." Thesis, University of Manchester, 1985. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.374582.
Повний текст джерелаJenkins, Gail. "Inducible macrolide and lincosamide resistance in Streptomyces lividans." Thesis, University of Leicester, 1990. http://hdl.handle.net/2381/35260.
Повний текст джерелаGomes, Cláudia, Puchol Sandra Martínez, Noemí Palma, Gertrudis Horna, Lidia Ruiz-Roldán, Maria J. Pons, and Joaquim Ruiz. "Macrolide resistance mechanisms in Enterobacteriaceae: Focus on azithromycin." Taylor & Francis, 2016. http://hdl.handle.net/10757/620710.
Повний текст джерелаSkinner, Michael Fredrick. "Biopharmaceutics and pharmacokinetics of the macrolide antibiotic Josamycin." Thesis, Rhodes University, 1992. http://hdl.handle.net/10962/d1003269.
Повний текст джерелаChung, Whasun Oh. "Macrolide resistance and its linkage to tetracycline resistance /." Thesis, Connect to this title online; UW restricted, 1999. http://hdl.handle.net/1773/9279.
Повний текст джерелаTavares, Júnior Eraldo Ramos. "Acesso à justiça e macrolides." Faculdade de Direito, 2015. http://repositorio.ufba.br/ri/handle/ri/17473.
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A presente dissertação se propõe à análise do acesso à justiça diante de uma nova conflituosidade social. Parece não existir dúvidas de que a tutela jurisdicional individual não é suficiente para a pacificação das relações conflituosas em massa, que assolam os tribunais de todo o país, através de milhares de ações repetitivas, com o mesmo objeto, e quase sempre, com o mesmo pedido. Aqueles que diariamente militam nos fóruns brasileiros têm a absoluta certeza de que questões relativas litígios seriados desafiam uma tutela jurisdicional diferenciada. Torna-se, então, imprescindível o estudo e desenvolvimento do tema, fazendo uma análise da Jurisdição e do Processo à luz do paradigma democrático, da compreensão do acesso à justiça na atualidade, bem como da tutela coletiva de direito, em especial dos direitos individuais homogêneos. Assim, o presente trabalho começa analisando os conceitos clássicos do processo e a sua repercussão da realidade jurídica brasileira atual. Após, procurou-se apontar os principais problemas que impedem o incremento do acesso à justiça, em especial diante de uma sociedade extremamente massificada, apresentando sugestões para superação dos problemas. Por fim, procurou tecer algumas considerações acerca do incidente de coletivização das demandas repetitivas, inserido no Novo Código de Processo Civil, aprovado pelo Senado Federal e pendente de envio para sanção presidencial. Essas são algumas questões discutidas no presente trabalho, que não tem o fito de esgotar a matéria, mas de fomentar e contribuir para a discussão do tema.
Blakey, S. "Synthesis of an advanced macrolide intermediate for the aplyronines." Thesis, University of Cambridge, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.596715.
Повний текст джерелаDalby, S. M. "Total synthesis of the macrolide core of (+)-spirastrellolide A." Thesis, University of Cambridge, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.598247.
Повний текст джерелаZhang, Ziyang. "A Platform for the Discovery of New Macrolide Antibiotics." Thesis, Harvard University, 2016. http://nrs.harvard.edu/urn-3:HUL.InstRepos:33493421.
Повний текст джерелаChemistry and Chemical Biology
Neeland, Edward George. "Selective reactions of 14-membered macrolides-a conformational approach using MM2 calculation." Thesis, University of British Columbia, 1987. http://hdl.handle.net/2429/29040.
Повний текст джерелаScience, Faculty of
Chemistry, Department of
Graduate
Rawson, D. J. "A total synthesis of (+)-(9S)-dihydroerythronolide A." Thesis, University of Cambridge, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.317889.
Повний текст джерелаGledhill, Adrian Paul. "Synthesis of polysubstituted fatty acids via thiophene intermediates." Thesis, Nottingham Trent University, 1991. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.304892.
Повний текст джерелаWood, Nicholas D. "Studies towards the synthesis of mycinolide III, mycinoic acids I & II and 1β,2α-dimethyl gibberellins". Thesis, University of Bristol, 1996. http://hdl.handle.net/1983/1322f2e7-4563-4a44-991b-a4bf89a5c81b.
Повний текст джерелаBower, S. "New methods in acyclic stereocontrol directed towards the synthesis of bafilomycin A1." Thesis, University of Cambridge, 1994. https://www.repository.cam.ac.uk/handle/1810/272787.
Повний текст джерелаKarray, Fatma. "Etude de la biosynthèse de l'antibiotique spiramycine par Streptomyces ambofaciens." Paris 11, 2005. http://www.theses.fr/2005PA112085.
Повний текст джерелаStreptomyces ambofaciens synthesizes the 16-membered macrolide antibiotic spiramycin. The biosynthetic gene cluster for spiramycin has been characterized in S. Ambofaciens. Sequence analysis of a region of more than 100 kb spanning the entire cluster revealed the presence of 50 genes, 41 of them being most probably involved in spiramycin biosynthesis, its regulation or resistance to the antibiotic. In order to study the role of the gene products in spiramycin biosynthesis, we constructed strains in which some genes were inactivated by in-frame deletion. For this purpose, we developed cassettes that can be easily excised by site-specific recombination. Two regulatory genes, srmR and srmS, were identified in the biosynthetic gene cluster. The disruption of each of these two regulatory genes eliminated spiramycin production while the over-expression of each of them increased three fold the level of spiramycin production. Expression analysis by RT-PCR for all the genes of the cluster in the wild type strain, in srmR and srmS deletion mutants and in the srmR, srmS double deletion mutant was performed. These results, together with complementation experiments, indicated that SrmR is required for srmS expression, SrmS being a pathway-specific activator that controls most of the spiramycin biosynthetic genes. Spiramycin is normally produced as a mixture of spiramycin I, II and III. Spiramycin I is the most active form of the antibiotic. We identified and inactivated the gene encoding the acetyltransferase responsible for the production of spiramycin II and III. The level of production of this mutant strain was further increased by over-expression of the regulatory gene srmR
MAYAN, BUSCARONS VALERIE. "Place des macrolides dans le traitement de premiere intention des bronchopneumopathies infectieuses communautaires de l'adulte." Aix-Marseille 2, 1990. http://www.theses.fr/1990AIX20076.
Повний текст джерелаWallwork, Benjamin, and n/a. "The Anti-Inflammatory Effect of Macrolide Antibiotics in Chronic Rhinosinusitis." Griffith University. School of Biomolecular and Biomedical Science, 2006. http://www4.gu.edu.au:8080/adt-root/public/adt-QGU20070201.160023.
Повний текст джерелаKönig, Ariane. "Genes for macrolide formation in rapamycin biosynthesis from Streptomyces hygroscopicus." Thesis, University of Cambridge, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.264158.
Повний текст джерелаMorel, Jean-David. "Mechanism underpinning the immunosuppressive effects of the mycobacterial macrolide mycolactone." Thesis, Sorbonne Paris Cité, 2018. http://www.theses.fr/2018USPCC316.
Повний текст джерелаMycolactone is a diffusible lipid produced by the human pathogen Mycobacteriumulcerans, the causative agent of a tropical skin disease called Buruli ulcer. Bacterial production of mycolactone in infected skin causes local tissue necrosis, while inducing immunosuppressive defects at the systemic level. When I started my PhD, the molecular mechanism(s) underpinning these effects were unknown. Over the course of my thesis, I contributed to demonstrate that mycolactoneis a novel inhibitor of the Sec61 translocon, a channel regulating the biogenesis of most secretedand membrane proteins in eukaryotic cells. Indeed, a single point mutation in the alpha subunit ofSec61 protected cells from the cytotoxic and immunosuppressive effects of mycolactone. I showed that mycolactone-mediated blockade of the Sec61 translocon efficiently prevents the synthesis ofkey immune receptors and signaling molecules, impeding the communication between immunecells that is required for the development of anti-mycobacterial immunity. Through a series of larges caleproteomic studies, I demonstrated that mycolactone is a broad-acting inhibitor of Sec61 and identified the Sec61 clients that are primarily down regulated by mycolactone in physiologicallyrelevant cell types. These analyses also allowed me to describe a unique stress response,encompassing elements of the unfolded protein response and integrated stress response, that isinduced upon protein translocation blockade and ultimately causes cell apoptosis. The Sec61 translocon has been proposed to play a role in other cell functions that require the retrograde transport of proteins across membranes, namely Endoplasmic Reticulum-Associated Degradation(ERAD), an essential process in protein quality control, and antigen export to the cytosol during cross-presentation, a pathway essential to the activation of adaptive immunity to intracellular pathogens and cancer. Using mycolactone, I showed that Sec61 blockade does not affect protein export to the cytosol in either of these pathways, arguing against Sec61 operating as are trotranslocon. Altogether, my work provided a molecular mechanism for the diverse effects of mycolactone in Buruli Ulcer patients, and thus for M. ulcerans virulence. Mycolactone representing the most potent Sec61 blocker identified to date, my studies also revealed the key importance of Sec61-mediated protein translocation in the regulation of immune responses and protein homeostasis
Arsic, Biljana. "Macrolide antibiotics as anti-bacterial and potential anti-malarial medicines." Thesis, University of Manchester, 2012. https://www.research.manchester.ac.uk/portal/en/theses/macrolide-antibiotics-as-antibacterial-and-potential-antimalarial-medicines(06d0269d-323f-4f46-9cf2-3eb7363b2796).html.
Повний текст джерелаWallwork, Benjamin. "The Anti-Inflammatory Effect of Macrolide Antibiotics in Chronic Rhinosinusitis." Thesis, Griffith University, 2006. http://hdl.handle.net/10072/367299.
Повний текст джерелаThesis (PhD Doctorate)
Doctor of Philosophy (PhD)
School of Biomolecular and Biomedical Sciences
Full Text
Lee, Miseon. "THE DISCOVERY OF NOVEL MACROLIDE ANTIBIOTICS THAT ADDRESS BACTERIAL RESISTANCE." Diss., Temple University Libraries, 2017. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/436439.
Повний текст джерелаPh.D.
Bacterial resistance is a formidable 21st-century global public health threat. If left unaddressed, we risk moving toward a “post-antibiotic era.” While resistance is a natural consequence of antibiotic use, the rate at which pathogenic bacteria have evaded multiple classes of drugs has markedly outpaced the introduction of new ones. New antibiotics are desperately needed to fill this void. Macrolides are one of the safest and most effective drug classes in medicine; however, resistance has compromised efficacy. To date, three generations have been developed with only the lattermost targeting bacterial resistance. Single next-generation macrolides will not keep pace with the inevitable onset of resistance; thus, there is a critical need to greatly accelerate the procurement of multiple future-generation antibiotics to tackle both current and future resistance mechanisms. My research is to meet this need by designing, synthesizing, and evaluating a novel, future-generation macrolide antibiotics that will serve as an armamentarium to be individually deployed on demand. In the previous research in Andrade group, we synthesized and evaluated various desmethyl ketolide analogs. The fact that 4-desmethyl telithromycin was fourfold less potent than telithromycin against A2058G mutants indicated replacing the 4-Me with hydrogen (i.e., desmethylation) to avoid a steric clash with the 2-amino group of G2058 was insufficient in rescuing bioactivity. Guided by MD simulation, we concluded a logical, superior alternative strategy was the replacement of the 4-Me group with one possessing a smaller vdW radius and capable of establishing favorable interactions with both wild-type and A2058G mutant ribosomes. Specifically, we reasoned that 4-fluoro solithromycin would be ideal candidate. The hypothesis was that the 4-fluoro moiety would engage in dipole-dipole interactions (C-F---H) with the exocyclic 2-amino group of guanine, which is based on accumulated evidence that strategic placement of organofluorine can strongly impact potency, selectivity, and physicochemical properties. In addition, the axially disposed of 4-fluorine would provide conformational stabilization from a gauche effect with the vicinal O5 group. The novel synthetic routes to unexplored desosamine analogs at the C3’-amino substituent to the macrolide antibiotic would play a role in bioactivity and resistance. Hofmann reaction was employed to execute the same 2,3-epoxide ring opening method without removing desosamine and re-glycosylating. This markedly reduces the steps, time, and cost involved in preparing novel desosamine-modified analogs. Significantly, this route enables the first synthesis of N,N’-disubstituted desosamine analogs from an epoxide, which was utilized to prepare novel analogs of clarithromycin. The application of in situ click chemistry toward the discovery of novel macrolide antibiotics first required the synthesis of suitable azide and aryl alkyne reactants. Alkyne partners were procured by commercial vendors or chemical synthesis. We targeted two logical, validated positions to tether the side chains, specifically N11 on the macrolactone and N3’ of desosamine. The first (N11) has been the most utilized. Moreover, extensive structure-activity relationships have revealed a four-carbon tether is ideal. Based on the solithromycin−E.coli X-ray structure, I designed, synthesized, and evaluated dehydro solithromycin, which possesses an (E)-alkene in the side-chain. The use of an unsaturated side chain would conformationally preorganize the bi-aryl side chain in order to pay the entropic penalty and thus favorably contribute to the overall binding. An insightful observation made from MD simulationed ribosomes bound with to solithromycin revealed that the interaction of the side-chain includes H-binding as well as π-stacking. The hypothesis was that employing tethered side-chains bearing motifs that maximize H-bonding and π-stacking would be superior antibiotics for treating resistant bacterial strains bearing erm¬-mediated N6 methyl and dimethylated ribosomes. To test this hypothesis, we developed various analogs with different alkynes by introducing different functional groups at the 3 and 5 positions on the aromatic ring. Another desosamine sugar modification is bis-azide. To date, the use of a two side chain strategy has not been reported. To access the requisite bis-azides, we employed a tactic the oxidative demethylation and alkylation of desosamine to afford bis-click solithromycin analogs.
Temple University--Theses
Chaume, Grégory. "Vers la synthèse totale de la griséoviridine, antibiotique de type streptogramine." Cergy-Pontoise, 2003. http://biblioweb.u-cergy.fr/theses/03CERG0256.pdf.
Повний текст джерелаChaume, Grégory Ardisson Janick. "Vers la synthèse totale de la griséoviridine, antibiotique de type streptogramine." [S.l.] : [s.n.], 2008. http://biblioweb.u-cergy.fr/theses/03CERG0256.pdf.
Повний текст джерелаLowden, A. S. "Studies on the biosynthesis of rapamycin." Thesis, University of Cambridge, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.340997.
Повний текст джерела周永昌 and Wing-cheong Louis Chow. "Modulation of acute inflammatory response caused by surgical trauma ina mastectomy model." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 1999. http://hub.hku.hk/bib/B31979622.
Повний текст джерелаButler, Aoife Patricia. "Studies directed towards the synthesis of bafilomycin Aâ†1." Thesis, University of Southampton, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.242251.
Повний текст джерелаHORMATALLAH, NOURJALIL. "Etat actuel et perspectives du traitement de maladies infectieuses a mycoplasma pneumoniae." Nancy 1, 1993. http://www.theses.fr/1993NAN1P072.
Повний текст джерелаBerque-Bestel, Isabelle. "Contribution a la synthese stereocontrolee de macrolides de type erythromycine." Paris 11, 1998. http://www.theses.fr/1998PA114803.
Повний текст джерелаHarper, Emily E., and Tara A. Jackson. "An Evaluation of Macrolide Drug-Drug Interactions for Quality in the Literature." The University of Arizona, 2011. http://hdl.handle.net/10150/623558.
Повний текст джерелаOBJECTIVES: To evaluate the quality of evidence in the literature substantiating major drug-drug interactions of the macrolide antibiotics azithromycin, clarithromycin, and erythromycin with digoxin, ergot alkaloids, and pimozide. METHODS: In this descriptive retrospective analysis, a list of articles reporting on each drug-drug interaction was compiled from the online databases Medline and International Pharmaceutical Abstracts, and the drug compendia Micromedex and Facts & Comparisons. The studies included in this analysis were primary literature reports, written in English, and consisted of human subjects. All studies included were evaluated using a 5-point quality of evidence scale developed in the Netherlands to assess drug-drug interactions (van Roon scale). This scale rates the study type from lowest to highest quality, from zero to four. Case reports were additionally analyzed using the Drug Interaction Probability Scale (DIPS). The DIPS tool uses 10 questions to evaluate the probability that an adverse event is caused by a drug-drug interaction. RESULTS: Thirty-seven studies met the selection criteria. There were 28 studies involving digoxin, two studies involving pimozide and seven studies involving ergot alkaloids. The mean quality of evidence score on the van Roon scale was 2.3 + 0.75, where digoxin studies had a score of 2.3 + 0.74, ergot alkaloids had a score of 1.9 + 0.38 and pimozide only had two studies with evidence scores of 2 and 4. Sixty-two percent of the studies reviewed were case reports. CONCLUSION: The reports substantiating some drug-drug interactions may be of low quality and few in number.
Chow, Wing-cheong Louis. "Modulation of acute inflammatory response caused by surgical trauma in a mastectomy model." Hong Kong : University of Hong Kong, 1999. http://sunzi.lib.hku.hk/hkuto/record.jsp?B23636464.
Повний текст джерелаKeller, Thomas Hugo. "Conformationally controlled reactions in 14-membered macrolides." Thesis, University of British Columbia, 1988. http://hdl.handle.net/2429/28844.
Повний текст джерелаScience, Faculty of
Chemistry, Department of
Graduate
Reader, Michael. "Studies towards the synthesis of the macrolide portion of ulapualide A." Thesis, University of Nottingham, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.294255.
Повний текст джерелаThirsk, Carl Edward. "Stereoselective routes to the total synthesis of the polyene macrolide viridenomycin." Thesis, Durham University, 2003. http://etheses.dur.ac.uk/3153/.
Повний текст джерела