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Dissertations / Theses on the topic '4-aminoquinoline'

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Published: 5 June 2025

Last updated: 2 August 2025

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1

Shone, Alison Emily. "The synthesis and metabolism of novel 4-aminoquinoline antimalarials." Thesis, University of Liverpool, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.443926.

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2

Fortuin, Elton E. "Novel aminoquinoline-polycyclic hybrid molecules as potential antimalarial agents." University of the Western Cape, 2014. http://hdl.handle.net/11394/4463.

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Magister Pharmaceuticae - MPharm<br>Plasmodium falciparum malaria continues to be a worldwide health problem, especially in developing countries in Africa and is responsible for over a million fatalities per annum. Chloroquine (CQ) is low-cost, safe and was the mainstay aminoquinoline derived chemotherapeutic agent that has been used for many years against blood-stage malaria. However, today the control of malaria has been complicated by increased resistance of the malaria parasite to existing antimalarial agents such as CQ. The primary cause of resistance is mutation in a putative ATP-powered

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3

Melo, Candice Soares de. "Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations." Master's thesis, University of Cape Town, 2006. http://hdl.handle.net/11427/6334.

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Includes bibliographical references.<br>The work presented in this thesis is two-fold: (i) development of single agents that provide inhibition of both the growth of malaria parasites and of tumour cells in vitro, and (ii) inclusion of these potential novel inhibitors in cyclodextrin host molecules in an attempt to render these dual drugs water-soluble. Of all the current clinically established antimalarials, the 4-aminoquinolines haveproven to be the most significant and efficacious for the treatment and prophylaxis of malaria. However, their efficacy has decreased by the spread of drug resis

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4

Hawley, Shaun Richard. "Studies on the chemical and physicochemical basis of 4-aminoquinoline accumulation, activity and resistance in Plasmodium falciparum malaria." Thesis, University of Liverpool, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.309903.

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5

Andayi, Warren Andrew. "Synthesis, antimalarial evaluation, Ç-hematin inhibition, and in silico and in vitro ADMET profiling of 4-aminoquinoline-hydroxypyridinone hybrids." Doctoral thesis, University of Cape Town, 2011. http://hdl.handle.net/11427/14824.

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Includes abstract.<br>With the aim of designing appropriate hybrid molecules as a strategy to fight drug resistant malaria parasites, 4-aminoquinoline-3,4-hydroxypyridinone hybrids were designed and synthesized. Their hypothesized mode of action was studied with respect to inhibition of hemozoin formation.

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6

Liebman, Katherine May. "New 4-Aminoquinoline Compounds to Reverse Drug Resistance in P. falciparum Malaria, and a Survey of Early European Antimalarial Treatments." PDXScholar, 2014. http://pdxscholar.library.pdx.edu/open_access_etds/2114.

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Intermittent fevers caused by Plasmodium parasites have been known for millennia, and have caused untold human suffering. Today, millions of people are afflicted by malaria each year, and hundreds of thousands die. Historically, the most successful synthetic antimalarial drug was chloroquine, as it was safe, inexpensive, and highly efficacious. However, plasmodial resistance to chloroquine now greatly limits its utility. Previously in our laboratories it has been shown that attachment of a "reversal agent moiety" to the side chain of chloroquine can result in the restoration of activity agains

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7

Mabotha, Tebogo E. "Haemozoin formation, effects of chloroquine on iron distribution in Plasmodium falciparum and the correlation of thermordynamic and structural factors with 4-aminoquinoline activity." Doctoral thesis, University of Cape Town, 2007. http://hdl.handle.net/11427/6326.

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Includes bibliographical references (leaves 178-191).<br>An interfacial method was developed in order to investigate the role lipids might play in haemozoin biosynthesis. Infrared and X-ray diffraction measurements demonstrated that β-haematin, a synthetic counterpart of haemozoin, forms efficiently at pentanol/water, octanol/water and lipid/water interfaces, but to a lesser extent at toluene/water interface under physiological conditions of pH and temperature and does not form at all in the absence of the interface.

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8

Antinarelli, Luciana Maria Ribeiro. "Atividade leishmanicida de derivados de quinolinas: 4-aminoquinolinas complexadas a esteroide e amodiaquina." Universidade Federal de Juiz de Fora (UFJF), 2013. https://repositorio.ufjf.br/jspui/handle/ufjf/5289.

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Souza, Isabela de Oliveira. "Síntese de derivados aminoquinolínicos e avaliação do efeito em protozoários." Universidade Federal de Juiz de Fora (UFJF), 2017. https://repositorio.ufjf.br/jspui/handle/ufjf/4655.

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Antinarelli, Luciana Maria Ribeiro. "Estudos in vitro, in vivo e in silico da atividade de derivados aminoquinolínicos em espécies de Leishmania relacionadas à Leishmaniose tegumentar americana." Universidade Federal de Juiz de Fora (UFJF), 2017. https://repositorio.ufjf.br/jspui/handle/ufjf/5599.

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11

Soares, Roberta Reis. "Avaliação da atividade antimalárica de análogos de 4-aminoquinolinas e 6-mercaptopurinas em modelo murino." Universidade Federal de Juiz de Fora (UFJF), 2013. https://repositorio.ufjf.br/jspui/handle/ufjf/4279.

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Submitted by isabela.moljf@hotmail.com (isabela.moljf@hotmail.com) on 2017-05-02T11:30:44Z No. of bitstreams: 1 robertareissoares.pdf: 1821120 bytes, checksum: 37f4636d8bd6ef3623072173760d6105 (MD5)<br>Approved for entry into archive by Adriana Oliveira (adriana.oliveira@ufjf.edu.br) on 2017-05-12T15:51:49Z (GMT) No. of bitstreams: 1 robertareissoares.pdf: 1821120 bytes, checksum: 37f4636d8bd6ef3623072173760d6105 (MD5)<br>Made available in DSpace on 2017-05-12T15:51:49Z (GMT). No. of bitstreams: 1 robertareissoares.pdf: 1821120 bytes, checksum: 37f4636d8bd6ef3623072173760d6105 (MD5) Pre

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12

Van, der Merwe Johannes Dawid. "Synthesis and antiplasmodial structure-activity relationships for some novel 4-aminoquinolines and 5-chlorobenzimidazoles." Master's thesis, University of Cape Town, 2004. http://hdl.handle.net/11427/6285.

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Includes bibliographical references.<br>Two novel 7-substituted 4-aminoalkylated quinolines, Nl,Nl-diethyl-N2-(7-trifuoromethylthio-4-quinolinyl)-1,2-ethanediamine 11 and Nt, Nl-diethyl-N2-(7-trifuoromethoxy-4-quinolinyl)-1,2-ethanediamine 12 were synthesized via a versatile 6-step route and their antiplasmodial activities against the chloroquine sensitive D10 strain of Plasmodium falciparum have been investigated in vitro. A quantitative structure activity analysis of these compounds showed an excellent correlation of log ICso, corrected for vacuolar accumulation, with log ß-haematin inhibito

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13

Vausselin, Thibaut. "Caractérisation de l'activité antivirale de dérivés de 4-aminoquinolines sur le virus de l'hépatite C." Thesis, Lille 1, 2013. http://www.theses.fr/2013LIL10078/document.

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L’infection par le virus de l’hépatite C (HCV) est un problème majeur de santé publique dont le traitement repose sur l’association d’interféron-α (IFN-α) pégylé et de ribavirine, toutes deux non spécifiques du HCV. Depuis 2011, des inhibiteurs de la protéase virale (boceprevir et telaprevir) ont amélioré l’efficacité du traitement, mais ceci reste limité au virus de génotype 1. De plus, le coût prohibitif et l’importance des leurs effets secondaires oblige au développement de nouveaux composés.La chloroquine, un antipaludique, est capable d’inhiber le HCV, mais son utilisation se complique pa

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14

Silva, Yolanda Karla Cupertino da. "Avaliação da atividade antinociceptiva e anti-inflamatória de novos protótipos de fármacos." Universidade Federal de Alagoas, 2014. http://www.repositorio.ufal.br/handle/riufal/1773.

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In this work, the evaluation of the antinociceptive and anti-inflammatory activities of two series of rationally designed derivative was performed. The first series belong to the class hydrazones thiophene derivative is formed by nine numbered 5a-i. The second is termed aminoquinolínicos BAQ, 7-Cl-MAQ, 2-CF3-MAQ e 7-CF3-MAQ, synthesized from structural modifications in the molecule chloroquine. The two series were synthesized and subjected to testing for antinociceptive activity (writhing test induced by acetic acid and testin

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15

Busa, Asanda V. "Synthesis, characterization, and molecular docking of novel 4-Aminoquinolines and Salicylaldimine complexes: evaluation as antimalarial and antitumor agents." University of the Western Cape, 2016. http://hdl.handle.net/11394/5711.

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Philosophiae Doctor - PhD (Chemistry)<br>Malaria remains a major global health problem and to date, hundreds of thousands of people die as a result of this disease every year. Malaria has been able to adapt and rebound despite various efforts made to combat the disease. The decrease in efficacy of many front-line drugs against malaria, due to increased resistance, prompts investigation into obtaining effective compounds that are able to overcome this resistance. This study investigated the synthesis, characterisation and biological evaluation of new quinoline (as antimalarial agents) as well a

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16

Dias, Rafael Mafra de Paula. "Síntese e avaliação biológica de derivados 4-aminoquinolínicos e 4-mercaptoquinolínicos." Universidade Federal de Juiz de Fora (UFJF), 2011. https://repositorio.ufjf.br/jspui/handle/ufjf/4296.

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17

Lima, Raquel de Meneses Santos Leite. "Síntese e avaliação antimalárica de novos derivados 4-aminoquinolínicos." Universidade Federal de Alagoas, 2014. http://www.repositorio.ufal.br/handle/riufal/1952.

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Diferent classes of antimalarial drugs have been used to treat malaria, but the emergence of resistant strains of Plasmodium these drugs have decreased their efficiency, causing serious public health problem in tropical areas of the world. In this context, we carried out the preparation and antimalarial evaluation of eleven organic compounds: 7-Cl-MAQ, MAQPZ, 7-Cl-MAQPZ, 2-CF3-MAQ, 7-CF3-MAQ, 7-CF3-MAQPZ, 2-CF3-MAQPZ, 8-Cl-MAQ, 7-Cl-BAQ, 7-CF3-BAQ, 8-Cl-BAQ. These were obtained from the same synthetic strategy, via nucleophilic aromatic substitution reaction between 4-chloroquinoline derivativ

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18

Machado, Rafael Carvalhaes. "Síntese de novos derivados de 1-(7-cloro-4-quinolinil) tiossemicarbazidas e semicarbazidas como potencias agentes antibacterianos e antiparasitários." Universidade Federal de Juiz de Fora (UFJF), 2011. https://repositorio.ufjf.br/jspui/handle/ufjf/4293.

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Submitted by Renata Lopes (renatasil82@gmail.com) on 2017-04-27T12:08:52Z No. of bitstreams: 1 rafaelcarvalhaesmachado.pdf: 4567959 bytes, checksum: d476d2158bd5cb7ad61d6470ecca1cee (MD5)<br>Approved for entry into archive by Adriana Oliveira (adriana.oliveira@ufjf.edu.br) on 2017-05-13T13:00:19Z (GMT) No. of bitstreams: 1 rafaelcarvalhaesmachado.pdf: 4567959 bytes, checksum: d476d2158bd5cb7ad61d6470ecca1cee (MD5)<br>Made available in DSpace on 2017-05-13T13:00:19Z (GMT). No. of bitstreams: 1 rafaelcarvalhaesmachado.pdf: 4567959 bytes, checksum: d476d2158bd5cb7ad61d6470ecca1cee (MD5) Previou

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Ikhmais, Balqis. "The role of NQO2 in tumour growth and response to therapeutic drugs." Thesis, University of Manchester, 2018. https://www.research.manchester.ac.uk/portal/en/theses/the-role-of-nqo2-in-tumour-growth-and-response-to-therapeutic-drugs(01ea58b0-c375-43c2-8074-3e0a7034bb21).html.

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NRH quinone oxidoreductase 2 (NQO2) is regarded as a mammalian Phase I detoxifying enzyme responsible for reducing quinones to hydroquinones. NQO2 is highly expressed in different types of cancer such as breast and prostate cancer suggesting its participatory role in the progression of these diseases. A potential reason for this is that NQO2 has the ability to modulate the stability of cyclin D1 and activity of NF-ÃÂoB and it has been shown that inhibition of NQO2, either genetically or pharmacologically, can alter the pattern of proliferation of cancer cells. However, the biological roles

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20

Dutta, Asish K. "Physicochemical characterization of NPC 1161C, an 8-aminoquinoline anti-malarial drug, and its inclusion complexes with cyclodextrins in solution state /." Full text available from ProQuest UM Digital Dissertations, 2006. http://0-proquest.umi.com.umiss.lib.olemiss.edu/pqdweb?index=0&did=1260798661&SrchMode=1&sid=4&Fmt=2&VInst=PROD&VType=PQD&RQT=309&VName=PQD&TS=1193423218&clientId=22256.

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21

Aderibigbe, Atim Blessing. "Macromolecular 4-aminoquinoline compounds as potential antimalarial drugs." Thesis, 2011. http://hdl.handle.net/10539/9130.

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4-Aminoquinolines have a long and successful history as antimalarials as they have provided a number of useful antimalarials. P. falciparum, a causative organism of the most deadly form of human malaria, is generally slow to develop resistance to these drugs. 4-Aminoquinoline derivatives appear to bind to nucleoproteins and interfere with protein synthesis in susceptible organisms; the drugs intercalate readily into double-stranded DNA and inhibit both DNA and RNA polymerase. In addition, 4-aminoquinolines are found to concentrate in parasites’ digestive vacuoles, thereby increasing the pH of

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22

Sola, I., S. Castellà, E. Viayna, et al. "Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal–antiplasmodial activity." 2015. http://hdl.handle.net/10454/7485.

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Yes<br>Dual submicromolar trypanocidal–antiplasmodial compounds have been identified by screening and chemical synthesis of 4-aminoquinoline-based heterodimeric compounds of three different structural classes. In Trypanosoma brucei, inhibition of the enzyme trypanothione reductase seems to be involved in the potent trypanocidal activity of these heterodimers, although it is probably not the main biological target. Regarding antiplasmodial activity, the heterodimers seem to share the mode of action of the antimalarial drug chloroquine, which involves inhibition of the haem detoxification proces

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23

Sola, I., A. Artigas, M. C. Taylor, et al. "Synthesis and biological evaluation of N-cyanoalkyl-, Naminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents." 2016. http://hdl.handle.net/10454/8940.

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Yes<br>Current drugs against human African trypanosomiasis (HAT) suffer from several serious drawbacks. The search for novel, effective, brain permeable, safe, and inexpensive antitrypanosomal compounds is therefore an urgent need. We have recently reported that the 4-aminoquinoline derivative huprine Y, developed in our group as an anticholinesterasic agent, exhibits a submicromolar potency against Trypanosoma brucei and that its homo- and hetero-dimerization can result in to up to three-fold increased potency and selectivity. As an alternative strategy towards more potent smaller molecule an

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Defaux, J., M. Sala, X. Formosa, et al. "Huprines as a new family of dual acting trypanocidal–antiplasmodial agents." 2011. http://hdl.handle.net/10454/7468.

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No<br>A series of 19 huprines has been evaluated for their activity against cultured bloodstream forms of Trypanosoma brucei and Plasmodium falciparum. Moreover, cytotoxicity against rat myoblast L6 cells was assessed for selected huprines. All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC50 values against T. brucei in the submicromolar to low micromolar range and selectivity indices for T. brucei over L6 cells of approximately 15, thus constituting interesting trypanocidal lead compounds. Two of these huprines were also found to be active against a

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Sola, I., A. Artigas, M. C. Taylor, et al. "Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines." 2014. http://hdl.handle.net/10454/7496.

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We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio.

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