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Dissertations / Theses on the topic 'Macrocyclic lactones'

Author: Grafiati

Published: 4 June 2021

Last updated: 5 February 2022

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1

Reather, James Andrew. "Late steps in the biosynthesis of macrocyclic lactones." Thesis, University of Cambridge, 2000. https://www.repository.cam.ac.uk/handle/1810/251730.

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2

Savill, Karen. "Investigations of 1,2,4-trioxanes as precursors of macrocyclic lactones." Thesis, Heriot-Watt University, 1993. http://hdl.handle.net/10399/1392.

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3

Munt, Simon Peter. "Radical cyclizations : an approach to the bryostatins." Thesis, University of Oxford, 1990. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.258009.

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4

Mowbray, Charles Eric. "Arcimycins : selective degradation and semi-synthesis." Thesis, University of Exeter, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.235913.

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5

Yilmaz, Esra [Verfasser]. "Metabolism of macrocyclic lactones and benzimidazoles in parasitic nematodes / Esra Yilmaz." Berlin : Freie Universität Berlin, 2019. http://d-nb.info/1201346665/34.

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6

Galazzo, Daniel. "A comparison of laboratory and field resistance to macrocyclic lactones in Haemonchus contortus /." Thesis, McGill University, 2004. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=82236.

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Sustainable parasite control in livestock depends on anthelmintic drugs. The nematode Haemonchus contortus, the most important intestinal parasite of sheep and goats has developed resistance to all classes of anthelmintics including moxidectin, the most potent of the macrocyclic lactones. Pyrosequencing was used to screen H. contortus laboratory and field strains for single nucleotide polymorphisms (SNPs) associated with resistance in three genes, and determine their involvement in field resistance to macrocyclic lactones. Specific SNPs increased in frequency in ivermectin/moxidectin la

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7

Godoy, Rosas Pablo. "Functional analysis of «Haemonchus contortus» P-glycoprotein-A and interaction with macrocyclic lactones." Thesis, McGill University, 2011. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=97122.

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Macrocyclic lactone (ML) resistance has been described in the parasitic nematode, Haemonchus contortus. One of the mechanisms involved could be the over expression of P-glycoproteins (Pgps) which are ABC transporters. These proteins may influence the concentration of MLs that reach their target. In H. contortus one ABC transporter that is overexpressed in ML resistant parasites is Pgp-A (HcPgp-A). The goal of this project was the expression of HcPgp-A, in transfected LLC-PK1 cells, and to see the effect of ivermectin and moxidectin on inhibition of rhodamine 123 transport by the transfected ce

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8

Ramcharitar, Steve Harrinarine. "The synthesis of macrocyclic ketones and lactones : approaches to naturally occurring macrolyde antibiotics." Thesis, University of Oxford, 1991. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.302875.

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9

Maiti, Tushar B. (Tushar Baran). "An Approach Towards the Total Synthesis of Clonostachydiol." Thesis, University of North Texas, 1995. https://digital.library.unt.edu/ark:/67531/metadc278800/.

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The syntheses of the unsymmetrical 14-membered bismacrolides have been reviewed. A total synthesis of clonostachydiol, the latest to join this family, has been attempted using trimethylsilyl acetylene as the builiding block and palladium catalyzed reactions for the formation of key bonds. The alkyne groups were introduced by Stille coupling of trimethylstannylethynyltrimethylsilane with an acid chloride for one fragment and by addition of lithiotrimethylsilyl acetylene to an aldehyde for the other. Lactic acid derivatives were chosen as starting materials for both fragments, thus introducing t

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10

Firas, Bassissi Mohamad. "Le rôle des lipides et des lipoprotéines plasmatiques dans le transport et la pharmacocinétique des lactones macrocycliques (aspects pharmacologiques et toxicologiques)." Toulouse 3, 2006. http://www.theses.fr/2006TOU30025.

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Les Lactones Macrocycliques (LMs) sont des antiparasitaires largement utilisé en médecine vétérinaire contre les endo et les ectoparasites. Nos travaux révèlent pour la première fois l'implication des lipoprotéines dans le transport plasmatique des 5 différentes lactones (Ivermectine, Doramectine, Moxidectine, Abamectine, prinomectine) chez les différentes espèces animales cibles y compris l'homme. De plus nous avons pu mettre en évidence l'impact des perturbations du profil plasmatique en lipides et lipoprotéines sur la pharmacocinétique et la distribution plasmatique des LMs. Au même titre n

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11

Lopes, Alberto Moura Mendes 1981. "Caracterização do gene codificante da subunidade alpha do canal de cloreto (GluCl alpha) possivelmente associado à resistência às lactonas macrocíclicas em Cochliomyia hominivorax(Diptera: Calliphoridae) = Characterization of the gene encoding the alpha subunit of the chloride channel (GluCl alpha) possibly associated with resistance to macrocyclic lactones in Cochliomyia hominivorax(Diptera: Calliphoridae)." [s.n.], 2013. http://repositorio.unicamp.br/jspui/handle/REPOSIP/316431.

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Orientador: Ana Maria Lima de Azeredo Espin<br>Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Biologia<br>Made available in DSpace on 2018-08-23T10:46:46Z (GMT). No. of bitstreams: 1 Lopes_AlbertoMouraMendes_M.pdf: 2739543 bytes, checksum: 13578f8ab684d7f2c1af2020305008a8 (MD5) Previous issue date: 2013<br>Resumo: O Brasil possui o maior rebanho bovino comercial do mundo, sendo este um dos setores de geração de renda mais importantes para o país. As infestações por ecto e endoparasitas estão entre os principais problemas que levam à diminuição da produtividade. Dent

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12

David, Marion. "Identification and functional characterization of an ABC transporter of Haemonchus contortus, the P-glycoprotein 13." Thesis, Toulouse 3, 2016. http://www.theses.fr/2016TOU30206/document.

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Les lactones macrocycliques (LM) sont des anthelminthiques (AH) à effet paralysant très utilisés chez les animaux et les humains contre les nématodes parasites. Cependant, leur succès thérapeutique est compromis par la résistance croissante aux LM, qui pourrait être en partie dû aux ABC transporteurs P-glycoprotéines (Pgps) sélectionnés et surexprimés chez les nématodes résistants aux LM. Dans ce travail, nous avons étudié plus précisément la P-glycoprotéine 13 du parasite de petits ruminants, Haemonchus contortus. Son orthologue chez le modèle nématode C. elegans, Cel-Pgp-13, est exprimé dans

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13

Albérich, Mélanie. "Impact de l'ivermectine sur les systèmes de détoxification des xénobiotiques : régulations chez l'hôte et chez le nématode." Thesis, Toulouse, INPT, 2014. http://www.theses.fr/2014INPT0102/document.

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Les infections par les nématodes gastro-intestinaux entrainent des baisses en productions animales et des pertes économiques majeures pour les éleveurs. Les lactones macrocycliques (LMs) sont parmi les antiparasitaires les plus utilisés dans la lutte contre les nématodes gastro-intestinaux en médecine vétérinaire. De part une utilisation intensive, des résistances aux LMs chez les parasites gastro-intestinaux se sont développées au sein des élevages du monde entier mettant en péril l'efficacité thérapeutique de ces molécules. Par ailleurs, le développement de nouveaux antiparasitaires est limi

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14

Forrester, Sean Geritt. "Characterization of a macrocyclic lactone receptor subunit from Haemonchus contortus." Thesis, McGill University, 2002. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=82872.

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Glutamate-gated chloride channels (GluCls) are the proposed site of action for macrocyclic lactone anthelminthics, such as IVM, and the milbemycins, such as MOX. The objective of this thesis was to determine whether Haemonchus contortus GluCls are important targets for these anthelminthics. To begin to address this we cloned a full length GluCl alpha-subunit cDNA from H. contortus (HcGluCla). This subunit shares a high homology with GluCl subunits from Caenhorhabditis elegans that have been shown to be important targets for IVM, suggesting that HcGluCla is also an IVM target. However, i

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15

Brown, Jesse. "Resorcylic Acid Lactone Thioesterases as Potential Biocatalysts." Thesis, Université d'Ottawa / University of Ottawa, 2019. http://hdl.handle.net/10393/38741.

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A key missing tool in the chemist’s toolbox is an effective biocatalyst for macrocyclization. Macrocycles limit the conformational flexibility of small molecules, often improving their ability to bind selectively and with high affinity to a target, making them a privileged structure in drug discovery. Resorcylic acid lactones (RALs) are a class of fungal macrocyclic polyketides that exhibit anti-cancer and anti-malarial activity among others. The thioesterases (TEs) found in the biosynthetic pathways for the zearalenone (Zea) and radicicol (Rdc) resorcylic acid lactones are responsible for mac

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16

FERREIRA, Fabr?cia Ferreira e. "Remiss?o da demodiciose canina ap?s o tratamento com a doramectina em diferentes protocolos." Universidade Federal Rural do Rio de Janeiro, 2016. https://tede.ufrrj.br/jspui/handle/jspui/1833.

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Submitted by Jorge Silva (jorgelmsilva@ufrrj.br) on 2017-06-26T18:12:15Z No. of bitstreams: 1 2016 - Fabr?cia Ferreira e Ferreira.pdf: 1846980 bytes, checksum: c127e17162c67e64b719801f92b0c6fc (MD5)<br>Made available in DSpace on 2017-06-26T18:12:15Z (GMT). No. of bitstreams: 1 2016 - Fabr?cia Ferreira e Ferreira.pdf: 1846980 bytes, checksum: c127e17162c67e64b719801f92b0c6fc (MD5) Previous issue date: 2016-03-23<br>Canine demodicosis is an inflammatory skin disease, frequently diagnosed in veterinary clinics, caused by the proliferation of mites of the species Demodex sp. In recent years

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17

Gerhard, Alexander Paul [Verfasser]. "The role of nematode P-glycoproteins in the mechanism of macrocyclic lactone resistance / Alexander Paul Gerhard." Berlin : Freie Universität Berlin, 2021. http://d-nb.info/1240674724/34.

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18

Sargison, Neil Donald. "Development of genetic crossing methods to identify genes associated with macrocyclic lactone resistance in the sheep nematode parasite, Haemonchus contortus." Thesis, University of Edinburgh, 2009. http://hdl.handle.net/1842/4395.

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There is a pressing need to develop strategies to reduce the emergence of macrocyclic lactone anthelmintic resistance in sheep flocks. Management practices aimed at maintaining anthelmintic susceptible nematodes in refugia while achieving a satisfactory level of production may prove to be useful. However, sensitive molecular tests are required to monitor the subtle effects of these practices on the frequency of resistance alleles within nematode populations. To-date, conventional studies of candidate genes coding for the known methods of action of macrocyclic lactone anthelmintics have produce

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19

LEYGUE, ESTREME NADINE. "Macrocylisation en series lactame, lactone et thiolactone : mise en evidence d'un tetralactame comme complexant selectif du calcium." Toulouse 3, 1987. http://www.theses.fr/1987TOU30124.

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20

Bliard, Christophe. "Synthèse d'hydrates de carbone, de sucres fluorés et d'analogues d'avermectine." Paris 11, 1987. http://www.theses.fr/1987PA112380.

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Les avermectines sont des composés antiparasitaires possédant une activité exceptionnelle ; ils sont obtenus par culture de microrganismes. Ce travail présente la synthèse de plusieurs analogues de l'avermectine-B₁a dans le but d'améliorer ses propriétés biologiques. Le premier chapitre présence une revue des propriétés biologiques, chimiques et structurales des avermectines ainsi que les études de métabolisme qui nous ont guidés dans le choix de nos analogues. Ceux-ci sont obtenus par dégradation partielle du composé naturel, protection sélective suivie ce qlycosylation avec différents analog

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21

Hutt, Jean. "Synthese d'analogues de la vitamine d::(3) : synthese chirale de composes polyhydroxyles." Université Louis Pasteur (Strasbourg) (1971-2008), 1986. http://www.theses.fr/1986STR13326.

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La transformation de la cfarvone en quatre diastereoisomeres precurseurs du cycle a des dihydrovitamines et dihydrotachysterols est decrite dans la premiere partie. Par couplage d'un acetylure derive des cycles c/d de la vitamine d::(3) avec la cetone precurseur du cycle a, puis sa formation du systeme dienique a l'aide de titane a basse valence nous avons obtenu des dihydrotachysterols majoritairement. D'un autre cote, l'utilisation de sulfoxydes optiquement actifs dans l'intention de creer des centres hydroxyles chiraux et son application a la synthese du fragment polyhydroxyle de l'amphoter

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22

BREUILLES, PASCAL. "Syntheses de dicetones un, quatre." Paris 6, 1988. http://www.theses.fr/1988PA066645.

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Trois nouvelles methodes de synthese de dicetones 1-4 sont proposees: la premiere par addition oxydante, a l'aide de sels de manganese et de cuivre, de cetones a des isopentenyl sulfones; la seconde par substitution allylique de sulfures ou de sulfones par des cetones enolisables; la troisieme par cycloaddition a une enone d'un nouveau reactif: la chloromethyl-2 allylphenylsulfone. Les produits de ces trois reactions sont des cetones comportant un groupe methylene en position 4 alors facilement transformees en dicetones par ozonolyse. L'utilite synthetique de ces trois methodes est illustree p

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23

Fenster, Erik. "Conformationally controlled reactions of unsaturated macrocyclic lactones and keto lactones." Thesis, 2000. http://hdl.handle.net/2429/10608.

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As part of a study of the chemistry of macrocyclic compounds in our laboratory, the 14-membered unsaturated lactones 29 and 30 were synthesized with high stereoselectivity (>16:1 EIZ) via the ring closing olefin metathesis (RCM) reaction of the open chain diene esters. The configuration of the double bond in these unsaturated lactones was determined by 1H homonuclear decoupling NMR experiments. Equilibrium studies demonstrated that the RCM reaction proceeds under thermodynamic control in the cases of 29 and 30. The keto lactones 67 and 68 were synthesized via the hydroboration of 30 fol

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24

Sharadendu, Anurag. "Synthesis and reactivity of macrocyclic β-keto lactones". Thesis, 1996. http://hdl.handle.net/2429/4760.

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As a part of a continuing study of the chemistry and conformational behaviour of macrocyclic β-keto lactones, 3-oxo-13-tetradecanolide (74) and 3-oxo-15-hexadecanolide (84) were synthesized via intra- and intermolecular alcoholysis of hydroxy Meldrum's acid derivatives. A number of 14- and 16-membered lactones, derived from 74 and 84 were used to investigate a series of alkylation and reduction reactions. [more abstract available in pdf]

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25

Wang, Chun-Chih, and 王俊智. "Cobalt-Catalyzed Highly Regio- and Stereoselective Reductive Ene-Ene and Ene-Yne Coupling Reactions: Application in the Synthesis of Lactones, Lactams and Macrocyclic Lactones." Thesis, 2004. http://ndltd.ncl.edu.tw/handle/32656386242429095336.

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博士<br>國立清華大學<br>化學系<br>92<br>In this work, we report two cobalt-catalyzed olefins dimerization modes: (a) reductive dimerization of conjugated alkenes to yield directly the saturated linear diesters, dinitrile, and disulfone 2a-2g, offering a more convenient method to the synthesis of adipic acid and, (b) cobalt-catalyzed head-to-tail dimerization of vinylarenes 4a-4l in good yields. On the other hand, we have recently developed a reaction mode of cobalt-catalyzed tail-to-tail reductive dimerization of conjugated alkenes. This provides an efficient and mild route for the corresponding saturate

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26

Bissonnette, Stéphane. "Recherche de la mutation ABCB1-1 chez des chiens exprimant des signes de toxicité subchronique suite à l'administration quotidienne de lactones macrocycliques." Thèse, 2008. http://hdl.handle.net/1866/7203.

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27

Demeler, Janina [Verfasser]. "The physiological site of action and the site of resistance to the macrocyclic lactone anthelmintics in sheep parasitic trichostrongyloid nematodes / vorgelegt von Janina Demeler." 2005. http://d-nb.info/978192788/34.

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28

Cusson, Jean-Philippe. "Étude de la cyclisation de lactones à 9 membres par réaction de métathèse et formation catalytique de liens benzyliques asymétriques." Thèse, 2017. http://hdl.handle.net/1866/19342.

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Préalablement, une synthèse de l’aliskiren, un inhibiteur de la rénine développé pour le traitement de l’hypertension, a été réalisée auprès du groupe Hanessian. Durant cette synthèse, une réaction clé de cyclisation par métathèse, menant à la formation de lactone à neuf membres, a été réalisée. Durant cette réaction, nous avons observé une différence de réactivité entre les diastéréomères, menant à la formation de monolactones et de dilactones, générant ainsi de l’intérêt pour l’étude des facteurs en cause. Le présent mémoire rapporte et détaille les résultats de cette analyse quant à la form

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