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Dissertations / Theses on the topic 'Antagonistic potential'

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Published: 3 June 2025

Last updated: 31 July 2025

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1

Tydings, Heather Anne. "Identification and Optimization of the Antagonistic Potential of Native Spinach Microbiota towards Escherichia coli O157:H7." Thesis, Virginia Tech, 2010. http://hdl.handle.net/10919/43364.

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Leafy greens such as spinach have been the object of several recent food-borne pathogen outbreaks. The purpose of this study was to isolate bacteria spinach epiphytic bacteria that inhibit growth of E. coli O157:H7, which we describe as antagonism. The mechanism of antagonism was investigated and we attempted to improve the antagonistic potential in vitro and on spinach leaves when cellobiose, a carbon source utilized by the antagonists but not E. coli O157:H7, was added. There were larger culturable populations of bacteria on the leaves of savoyed cultivars compared to flat. From the isolated

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2

Kumar, Pratheesh [Verfasser]. "Study on Antagonistic and Growth Promotion Potential of Certain Exo and Endophytic Bacteria of Mulberry (Morus SPP.) : Biological control / Pratheesh Kumar." München : GRIN Verlag, 2019. http://d-nb.info/118869961X/34.

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3

Mokashi, Alison Ann. "Thymoquinone the evaluation of its cytotoxic potential effects on P53 status and the cell cycle in various cancer cell lines /." Lexington, Ky. : [University of Kentucky Libraries], 2004. http://lib.uky.edu/ETD/ukyphsc2004t00141/Mokashi.pdf.

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Thesis (M.S.)--University of Kentucky, 2004.<br>Title from document title page (viewed June 21, 2004). Document formatted into pages; contains viii, 76 p. : ill. Includes abstract and vita. Includes bibliographical references (p. 69-74).

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4

Jansen, Malin Insa [Verfasser], and Frank [Akademischer Betreuer] Lyko. "Phenotyping the potential antagonistic knock-out of the chromatin remodeler EZH2 and CHD7 in neural stem cells and the adult brain / Malin Insa Jansen ; Betreuer: Frank Lyko." Heidelberg : Universitätsbibliothek Heidelberg, 2020. http://d-nb.info/1222517612/34.

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5

Jansen, Malin [Verfasser], and Frank [Akademischer Betreuer] Lyko. "Phenotyping the potential antagonistic knock-out of the chromatin remodeler EZH2 and CHD7 in neural stem cells and the adult brain / Malin Insa Jansen ; Betreuer: Frank Lyko." Heidelberg : Universitätsbibliothek Heidelberg, 2020. http://d-nb.info/1222517612/34.

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6

Pattison, Anthony Barry [Verfasser]. "The importance of the antagonistic potential in the management of populations of plant-parasitic nematodes in banana (Musa AAA) as influenced by agronomic factors / Anthony Barry Pattison. Landwirtschaftliche Fakultät." Bonn : Universitäts- und Landesbibliothek Bonn, 2011. http://d-nb.info/1016599587/34.

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7

Ranjan, Nilabh [Verfasser], Karlheinz [Akademischer Betreuer] Friedrich, Aria [Akademischer Betreuer] Baniahmad, and Gerhard [Akademischer Betreuer] Müller-Newen. "A study on the antagonistic targeting of thymic stromal lymphopoietin (TSLP) as a potential therapeutic strategy for Asthma bronchiale / Nilabh Ranjan. Gutachter: Karlheinz Friedrich ; Aria Baniahmad ; Gerhard Müller-Newen." Jena : Thüringer Universitäts- und Landesbibliothek Jena, 2016. http://d-nb.info/1081366915/34.

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8

Rayat, Harnak Singh. "The synthesis of potential steroid receptor antagonists." Thesis, University of Warwick, 1995. http://wrap.warwick.ac.uk/56111/.

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The first section of this thesis presents a review of the literature on endocrine hormones, synthetic steroids, and synthetic steroid receptor antagonists. Particular emphasis is placed upon the estrogen, progesterone and glucocorticoid activity of these compounds. The structure, activity and preparation of some progesterone/glucocorticoid receptor antagonists is also reviewed. The second section of this thesis presents a route for the synthesis of 19-aryl substituted androstanes. These compounds have been designed to explore their potential antiprogestational and antiglucocorticoid activity.

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9

Slaughter, Kimari. "Synthesis and Development of Potential CB1 Receptor Neutral Antagonists." ScholarWorks@UNO, 2012. http://scholarworks.uno.edu/td/1483.

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Cannabis and its derivatives have been used for both medicinal and recreational purposes. The study of this plant led to the discovery of over 60 cannabinoids, found exclusively in cannabis, that contribute to the behavioral effects of cannabis use, the most common is delta-9-tetrahydrocannabinol. Cannabinoid receptors function to increase activity in the mesolimbic dopamine reward system. Dopamine is a neurotransmitter that plays a major role in addition and its regulation plays a crucial role in mental and physical well-being. There is evidence that CB1 receptors are important to the reinfor

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Quintero, Emmeris Ivan Quintero. "Insumos e indicadores Biol?gicos em Agrossistemas com Bananeiras." Universidade Federal Rural do Rio de Janeiro, 2010. https://tede.ufrrj.br/jspui/handle/jspui/1165.

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Submitted by Sandra Pereira (srpereira@ufrrj.br) on 2016-08-17T13:45:07Z No. of bitstreams: 1 2010 - Emmer?s Ivan Q. Quintero.pdf: 1261300 bytes, checksum: 0078bde3a7d0a80eea89948870dd7901 (MD5)<br>Made available in DSpace on 2016-08-17T13:45:07Z (GMT). No. of bitstreams: 1 2010 - Emmer?s Ivan Q. Quintero.pdf: 1261300 bytes, checksum: 0078bde3a7d0a80eea89948870dd7901 (MD5) Previous issue date: 2010-03-29<br>Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior - CAPES<br>Studies were performed in the experimental area of Embrapa Agrobiologia, region - RJ, in order to evaluate the asso

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11

Derrick, Ian. "Cinnamoylamino and methoxyfumaroylamino derivatives of epoxymorphinans - potential irreversible ligands for opioid receptors." Thesis, University of Bristol, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.336849.

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12

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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13

Sepcic, Kelly Hall. "Sythesis of mazindol derivatives as potential irreversible antagonists of cocaine and other stimulants." Thesis, Georgia Institute of Technology, 1992. http://hdl.handle.net/1853/26819.

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14

ARRIDU, ANTONELLA. "Design and synthesis of new potential anticancer agents and high-selective A2B antagonists." Doctoral thesis, Università degli Studi di Cagliari, 2016. http://hdl.handle.net/11584/266708.

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The synthesis of antitumor agents covers a large part of current medicinal chemistry efforts. This thesis mainly focuses on the synthesis of different scaffolds as new potential anticancer agents. Two different approaches were applied: a hybrid concept and a rational based drug design. In the first case, the hybrid concept is useful since it allows combining multiple active scaffolds in a unique molecule. As a consequence, several targets could be hit simultaneously, making this solution particularly attractive for multi-factorial diseases like cancer. Within this category, several isatin-thi

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15

Picken, Paula. "The synthesis of endothelin analogues : potential application to immunoassay and receptor antagonist development." Thesis, Queen's University Belfast, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.318826.

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16

Almgren, Colleen Marie D. V. M. Ph D. "The potential role of potent prolactin antagonists as chemotherapeutics for human cancers: an evaluation of select prolactin antagonists in human breast cancer cells." The Ohio State University, 2005. http://rave.ohiolink.edu/etdc/view?acc_num=osu1104778150.

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17

Harrold, Marc W. "Part 1, synthesis of trimetoquinol analogs as potential thromboxane A2 receptor antagonists ; Part 2, synthesis of permanently charged and permanently uncharged dopamine antagonists /." The Ohio State University, 1987. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487584612165271.

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18

Almgren, Colleen Marie. "The potential role of potent prolactin antagonists as chemotherapeutics for human cancers an evaluation of select prolactin antagonists in human breast cancer cells /." Connect to this title online, 2005. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=osu1104778150.

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Thesis (Ph. D.)--Ohio State University, 2005.<br>Title from first page of PDF file. Document formatted into pages; contains xx, 199 p.; also includes graphics (some col.) Includes bibliographical references (p. 178-199).

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19

Lewis, John F. "The design and synthesis of sulphur heterocycles with potential as #gamma#- aminobutyric acid antagonists." Thesis, Staffordshire University, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.314152.

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20

Kang, Yuanxi, and 康元曦. "Mechanism study of novel CCR5 antagonists and their potential as anti-HIV-1 microbicides." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2012. http://hub.hku.hk/bib/B47849393.

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R5-tropic HIV-1 is predominantly transmitted during unprotected sexual contacts, rendering CCR5 antagonist as an attractive agent not only for antiretroviral therapy but also for prevention. Here, we report two 1,3,3,4-tetrasubstituted pyrrolidine embodied compounds, TD-0232 and TD-0680, as novel small molecule CCR5 antagonists and investigate their specificities, potencies and underlying mechanisms. We found that both TD-0232 and TD-0680 inhibited a diverse group of R5-tropic HIV-1 and SIV strains in both single-cycle infectivity assays and live viral PBMC assays. When compared to other CCR5

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21

Kent, Charles. "The potential of the superoxide dismutase inhibitor, diethyldithiocarbamate as an adjuvant to radiotherapy." Doctoral thesis, University of Cape Town, 1990. http://hdl.handle.net/11427/26550.

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It has long been known that oxygen has the potential to be toxic to biologic systems and that this toxicity is not due to oxygen itself, but due to the production of oxygen radicals. One of these potentially toxic radicals, superoxide (O₂⁻) can be generated as a result of ionizing radiation, and if not adequately removed can proceed to cause cell damage. Superoxide dismutase (SOD) is one of the key enzymes involved in the defence against oxygen toxicity. SOD activity can be inhibited by diethyldithiocarbamate (DOC), a powerful copper chelator. If inhibition of SOD by DOC increases the lifetime

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22

McKeveney, Declan, and n/a. "The Solid-Phase Combinatorial Synthesis of 2,6,9- Trisubstituted Purines as Potential Adenosine A3 Receptor Antagonists." Griffith University. School of Science, 2005. http://www4.gu.edu.au:8080/adt-root/public/adt-QGU20050830.120105.

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Purines as a class of compounds have been implicated in many biological systems, including as adenosine receptor antagonists. A method of synthesising 2,6,9-trisubstituted purines would be useful to produce small libraries of compounds for probing adenosine receptor selectivity. A library of trisubstituted purines has been achieved using a solid-phase methodology. The electronic properties of the substrate were found to result in difficulties with the loading of substrate onto the resin. Theoretical calculations provided the basis for mono-substitution in order to activate the substrate. This

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23

McKeveney, Declan. "The Solid-Phase Combinatorial Synthesis of 2,6,9- Trisubstituted Purines as Potential Adenosine A3 Receptor Antagonists." Thesis, Griffith University, 2005. http://hdl.handle.net/10072/367926.

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Purines as a class of compounds have been implicated in many biological systems, including as adenosine receptor antagonists. A method of synthesising 2,6,9-trisubstituted purines would be useful to produce small libraries of compounds for probing adenosine receptor selectivity. A library of trisubstituted purines has been achieved using a solid-phase methodology. The electronic properties of the substrate were found to result in difficulties with the loading of substrate onto the resin. Theoretical calculations provided the basis for mono-substitution in order to activate the substrate. This

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24

Jali, Abdulmajeed. "DISCOVERY OF MOR SELECTIVE, REVERSIBLE OPIOID ANTAGONIST FOR POTENTIAL USE IN TREATMENT OF DRUG DEPENDENCE." VCU Scholars Compass, 2017. http://scholarscompass.vcu.edu/etd/5020.

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Abstract DISCOVERY OF MOR SELECTIVE, REVERSIBLE OPIOID ANTAGONIST FOR POTENTIAL USE IN TREATMENT OF DRUG DEPENDENCE Abdulmajeed M. Jali, M.S. A thesis submitted in partial fulfillment of the requirements of Master of Science at Virginia Commonwealth University. Virginia Commonwealth University, 2017 Director: Dana E. Selley, Ph. D., Department of Pharmacology and Toxicology Opioid dependence/addiction is a major public health problem that is associated with multiple health and social costs. Pharmacotherapeutic treatment has been relatively effective, but the risk of relapse after treatment rem

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25

Markovich, Kimberly M. "Part 1. Synthesis of fluorinated catecholamine derivatives as potential adrenergic stimulants and thromboxane A? antagonists ; Part 2. Synthesis of hydrazinium analogs of dopamine agonists and antagonists /." The Ohio State University, 1991. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487687485808709.

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26

Perrin, Véronique. "Synthèse et caractérisation pharmacologique de nouveaux antagonistes potentiels des récepteurs du thromboxane A2." Lyon 1, 1996. http://www.theses.fr/1996LYO10314.

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Le thromboxane a#2 est un puissant constricteur des muscles lisses vasculaires et respiratoires ainsi qu'un agent de l'agregation plaquettaire. Il est implique dans des pathologies respiratoires, cardiovasculaires et renales. Compte tenu de l'etude des caracteristiques communes a de nombreux antagonistes connus, notre but etait de preparer des antagonistes des recepteurs du thromboxane a#2 possedant une structure 2-azanorbornane et ayant une fonction sulfone sur l'atome d'azote, ainsi que la chaine superieure, plus ou moins modifiee, des prostaglandines. Les differentes molecules obtenues ont

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27

Philion, Vincent. "The screening of potential fungal antagonists of pseudothecial formation by the apple scab pathogen : Venturia inaequalis." Thesis, McGill University, 1994. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=22791.

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In 1992, a research program was initiated to select suitable antagonists against the saprophytic (or winter) phase of the apple scab pathogen, Venturia inaequalis. An improved method for the mass screening of a vast collection of fungi was developed for this purpose. Some of the previously reported criteria such as leaf rheology and overwintering structure production proved unreliable or fastidious and cannot be used for in vitro antagonist selection. The main antagonism selection criterium retained was the in vitro inhibition of ascospore formation. To measure ascospore production, a simplifi

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28

Jaffar, M. "On the synthesis and stereochemistry of novel phenindamine and histryl analogues as potential H₁-histamine antagonists." Thesis, University of Bath, 1993. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.332338.

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29

Natividad, Gaudencio M. "Isolation and chemical and pharmacological characterization of potential trace amine-associated receptor antagonist from plant sources." Thesis, Cardiff University, 2010. http://orca.cf.ac.uk/54392/.

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The present study describes the preliminary evaluation of Philippine medicinal plants <italic>Artemisia vulgaris, Chrysanthemum coronarium, Moringa oleifera, Sesbania grandiflora</italic> and <italic>Vitex negundo</italic> for their antagonistic activity at selected biogenic amine receptors on smooth muscle of the airways, gastrointestinal tract and vascular system. The antagonistic activity of these plants were studied against dose-response curves for contractions of the guinea pig ileum, trachea and aorta to 5-hydroxytryptamine (5-HT2 receptors), methacholine (M3 muscarinic receptors), hista

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30

Nurit, Josiane. "Réactivité de l'hydroxyle secondaire du 1-phényl-glycérol. Application à la synthèse de 3-alcoyl-1-acyl glycérols, antagonistes potentiels de leucotriènes." Montpellier 1, 1992. http://www.theses.fr/1992MON13506.

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31

Smith, Stuart Ernest. "Excitatory amino acid antagonists and related agents as potential therapies in focal cerebral ischaemia in the rat." Thesis, King's College London (University of London), 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.281943.

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32

Puget, Alain. "Synthèse et évaluation pharmacologique de peptidomimétiques à structure indoliques antagonistes potentiels de la LHRH." Nantes, 2003. http://archive.bu.univ-nantes.fr/pollux/show.action?id=5e12c32c-3555-4135-839c-e7aae5552d72.

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Les analogues de la LHRH, aussi bien agonistes qu'antagonistes, peuvent être employés dans le traitement de nombreuses pathologies hormonodépendantes. Le développement d'antagonistes peptidomimétiques est un axe majeur de la recherche dans ce domaine. L'usage des antagonistes permet d'éliminer le phénomène de 'flare-up' observé chez les agonistes et la recherche de structures non peptidiques devrait conduire à la mise au point de médicaments utilisables par voie orale. Nous basant sur des études structurales de la LHRH et de ses analogues, nous avons conçu trois séries de molécules de structur

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33

Puget, Alain Le Baut Guillaume. "Synthèse et évaluation pharmacologique de peptidomimétiques à structure indoliques antagonistes potentiels de la LHRH." [S.l.] : [s.n.], 2003. http://theses.univ-nantes.fr/thesemed/DOCpuget.pdf.

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34

Chen, Wenxiong, and 陈文雄. "Potential interventional modalities on neurodevelopmental and neurodegenerative diseases: in vivo and invitro study." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2009. http://hub.hku.hk/bib/B43941072.

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35

Champagne, Annie. "Potentiel antagoniste des bactéries lactiques épiphytes de plantes fourragères contre le développement des clostridies dans l'ensilage." Thesis, Université Laval, 2007. http://www.theses.ulaval.ca/2007/24347/24347.pdf.

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36

Riveron, Véronique. "Synthèse et étude de nouveaux antagonistes potentiels du thromboxane A2 et de la prostaglandine H2 faisant intervenir un squelette 2-azanorbornane." Lyon 1, 1993. http://www.theses.fr/1993LYO10293.

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Le thromboxane a2 est un puissant agent constricteur des muscles lisses et un agregant des plaquettes sanguines. Il intervient dans des pathologies cardiovasculaires et respiratoires. Au vu de la litterature, notre but etait d'obtenir des antagonistes des recepteurs du thromboxane a2 ayant un squelette 2-azanorbornane et incluant une fonction sulfonee sur l'azote, ainsi que la chaine alpha des prostaglandines (6 ou 7 atomes de carbone). La molecule finale comportant la chaine 5-hexenoique, a ete testee sur les recepteurs vasculaires chez le rat conscient normo-tendu, par observation des repons

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37

Traversa, Christel. "Synthèse et étude de nouveaux antagonistes potentiels du thromboxane A2 à partir d'aza-7-norbornadiènes." Lyon 1, 1994. http://www.theses.fr/1994LYO10305.

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Le thromboxane a#2 est un puissant agent constructeur des muscles lisses et un agregant plaquettaire implique dans l'hypertension arterielle, l'infarctus du myocarde, l'asthme et des maladies renales. Nous basant sur des caracteristiques communes a un grand nombre d'antagonistes connus, nous avons synthetise des molecules presentant comme structure de base un squelette 7-azanorbornane et la chaine superieure, complete ou non, des prostaglandines. Le squelette est obtenu par une reaction de diels-alder thermique entre le pyrrole 1-carboxylate de tertiobutyle et l'acetylene dicarboxylate de meth

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38

Han, Rui [Verfasser]. "Identification of triptolide as a potential aryl hydrocarbon receptor antagonist in human T cells and keratinocytes / Rui Han." Kiel : Universitätsbibliothek Kiel, 2011. http://d-nb.info/1020245166/34.

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39

Hoxha, M. "THE POTENTIAL THERAPEUTIC ROLE OF MONTELUKAST AND NEW HYBRID AGENTS, TXA2 ANTAGONIST-COX-2 INHIBITORS IN CARDIOVASCULAR EVENTS." Doctoral thesis, Università degli Studi di Milano, 2016. http://hdl.handle.net/2434/347148.

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The main target of my PhD research project was to explore new alternatives to reduce the cardiovascular (CV) risk targeting the arachidonic acid metabolites. Hence, I have been part of two different projects, one studying multitarget compounds with balanced COXIB and TP receptor antagonist properties, and the other evaluating the potential role of a leukotriene (LT) antagonist drug such as montelukast in improving the CV outcome. In reference to the first project, new multitarget compounds were synthesized at the University of Turin, by substituting the carboxylic function of Lumiracoxib.

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McShane, Laura Majella. "The potential of novel glucagon receptor antagonists alone and in combination with other peptides for the treatment of diabetes." Thesis, Ulster University, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.652015.

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The ever increasing prevalence of diabetes mellitus worldwide warrants the need for new and effective treatment options. Although decades of research have primarily focused on insulin deficiency as the underlying defect in this disorder, a new wave of exploration in recent years has underpinned the role of hyperglucagonaemia as the key driving force behind hepatic glucose production and exacerbated hyperglycaemia in these patients. In an effort to antagonise glucagon signalling and investigate the potential benefits of glucagon ablation therapy, novel glucagon derived peptide antagonists were

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Senthilkumar, B. "Synthesis of small molecule PIP3 antagonists as potential anticancer agents and metal-catalyzed C-H oxidation of cyclotriveratrylene derivatives." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2015. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2003.

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Massip, Stéphane. "Synthèse de nouvelles xanthines, dérivées de 2-amino-2-oxazolines, antagonistes potentiels des récepteurs de l'adenosine." Bordeaux 2, 2005. http://www.theses.fr/2005BOR21206.

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Ce travail de thèse nous a permis de synthétiser un grand nombre de nouveaux dérivés de type 1- ou 3-[2-hydroxy-3-aryloxypropyl]xanthines. Ces composés ont été obtenus à partir d'un synthon original de type amidine, les 2-amino-2-oxazolines. Les différentes voies réaxtionnelles nous ont conduit à des diaminouraciles intermédiaires diversement substitués dont les possibilités réactionnelles nous ont permis l'accès à plus de 60 nouvelles xanthines et analogues. Différentes stratégies de synthèse ont été développées pour accéder à de nouvelles xanthines 3 différemment substituées en position 1 et

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43

Guillon, Jean. "Contribution à l'étude de nouvelles pyrrolo [1,2-α] quinoxalines : potentiels antagonistes non-peptidiques du récepteur au glucagon". Caen, 1996. http://www.theses.fr/1996CAEN4058.

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Fournet, Steven P. "High Resolution X-ray Diffraction Analysis of CB1 Receptor Antagonists as a Means to Explore Binding Affinity." ScholarWorks@UNO, 2013. http://scholarworks.uno.edu/td/1737.

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Abstract Charge density studies have been conducted on ten CB1 cannabinoid receptor antagonists via high resolution x-ray crystallography. Bond critical point values and various other properties derived from these studies including the electrostatic potential were analyzed in correlation to the affinity of each compound with the CB1 receptor. Correlation/anti-correlation was found between several properties and Ki. The data was also interpreted by principal component analysis with three principal components accounting for 85% of the data variation. Data mining was limit due to the low sample c

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45

Smith, Andra Marie Carleton University Dissertation Psychology. "A profile of the pharmacotherapeutic potential of the dopamine autoreceptor antagonist ( - )-DS121 using the self-administration paradigm in the rat." Ottawa, 1993.

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46

Obeng, Samuel. "Design, Synthesis, and Biological Screening of Selective Mu Opioid Receptor Ligands as Potential Treatments for Opioid Addiction." VCU Scholars Compass, 2017. http://scholarscompass.vcu.edu/etd/4771.

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Today, more Americans die each year because of drug overdoses than are killed in motor vehicle accidents. In fact, in 2015, more than 33,000 individuals died due to an overdose of heroin or prescription opioids. Sadly, 40-60 % of patients on current opioid addiction treatment medications relapse. Studies have shown that the addiction/abuse liability of opioids are abolished in mu opioid receptor (MOR) knock-out mice; this indicates that the addiction and abuse liability of opioids are mainly mediated through MOR. Utilizing the “message-address concept”, the our laboratory reported a novel non-

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Millet, Régis. "Conception, synthese et etude pharmacologique de ligands, antagonistes potentiels des recepteurs nk1 et nk2, de la substance p et de la neurokinine a (doctorat : pharmacochimie)." Lille 2, 1999. http://www.theses.fr/1999LIL2P015.

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Akue-Gedu, Rufine. "Conception rationnelle et synthèse d'inhibiteurs potentiels de la topoisomérase II : synthèse complète de la camptothécine." Lille 2, 2004. http://www.theses.fr/2004LIL2S013.

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Les topoisomérases sont la cible de certains médicaments anticancéreux. L’ellipticine et ses dérivés sont de bons modèles d’inhibiteurs de la topoisomérase II. Ils interagissent aussi directement avec l’ADN par intercalation. L’acétate de 2-N-méthyl-9-méthoxyelliptinium (CEPTIUM*) a été utilisé en clinique dans le traitement du cancer du sein. Il est retiré du marché à cause de sa forte toxicité. Le but de notre travail est de concevoir et de synthétiser de nouvelles molécules analogues de l’ellipticine en modifiant sa structure par pharmacomodulation. Nous proposons également une synthèse com

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49

Williams, Brett H. "Design and synthesis of 3-[N-(cyclopropylmethyl) amino]-7-(methoxy or hydroxy)-2, 2-dimethyl-1-tetralone analogs as potential opioid receptor antagonists." Scholarly Commons, 2004. https://scholarlycommons.pacific.edu/uop_etds/591.

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A series of 3-aminotetralins were synthesized as potential opioid antagonists. Each proposed target compound was based on a 3-(mono- or dialkylamino )-7 -(hydroxy or methoxy)-2, 2-dimethyl-1-tetralone parent structure. Three synthetic schemes were developed utilizing the common intermediate, ethyl3-benzylamino-2, 2-dimethyl-4-(4- methoxyphenyl)butyrate 3. In Scheme I, compound 3 was modified through a series of six steps to obtain 3-(N-methyl-N-cyclopropanecarboxamido )-7 -methoxy-2, 2-dimethyl- 1-hydroxy-1-phenyltetralin (9). To carry out further synthetic steps on the intermediate 9 required

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50

Herrmann, Ulrike [Verfasser], Olaf [Akademischer Betreuer] Prante, and Peter [Gutachter] Gmeiner. "Evaluation of Neurotensin Receptor-1 Antagonists as Potential Radiotracers for the Therapy of Pancreatic Adenocarcinoma / Ulrike Herrmann ; Gutachter: Peter Gmeiner ; Betreuer: Olaf Prante." Erlangen : Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), 2020. http://d-nb.info/1213533260/34.

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