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In silico drug design of potential novel anti malarial agents /Thovarai, Vishal. January 2009 (has links)
Thesis (M.S.)--Rochester Institute of Technology, 2009. / Typescript. Includes bibliographical references (leaves 45-49).
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Gene expression profiling of polyamine-depleted Plasmodium falciparumDhoogra, Minishca.. January 2007 (has links)
Thesis (M.Sc.)(Biochemistry))-University of Pretoria, 2007. / Summary in English. Includes bibliographical references. Available on the Internet via the World Wide Web.
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Kinetic analysis of a recombinantly expressed Plasmodium falciparum dihydrofolate synthase-folylpolyglutamate synthaseHuman, Esmaré January 2007 (has links)
Thesis (MSc Natural and Agricultural Sciences (Biochemistry))-University of Pretoria, 2007. / Summary in English and Afrikaans. Includes bibliographical references. Available on the Internet via the World Wide Web.
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Automated structural annotation of the malaria proteome and identification of candidate proteins for modelling and crystallization studiesJoubert, Yolandi. January 2007 (has links)
Thesis (M.Sc.)(Biochemistry))-University of Pretoria, 2007. / Summary in English. Includes bibliographical references. Available on the Internet via the World Wide Web.
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Discovery and characterization of polyamine analogues as inhibitors of the Plasmodium falciparum polyamine pathway using cheminformaticsDe Bruin, Jurgens Jacobus.. January 2009 (has links)
Thesis (M.Sc.)(Biochemistry))--University of Pretoria, 2008. / Includes summary.
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In silico structural characterisation of Plasmodium falciparum dihydro-6-hydroxymethylpterin pyrophosphokinase dihydropteroate synthase (PPPK-HPS)De Beer, Tjaart Andries Petrus. January 2005 (has links)
Thesis (M.Sc.)(Biochemistry)--University of Pretoria, 2005. / Title from opening screen (viewed March 27, 2006). Includes summary.
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Artemisia annua L.: produção de biomassa, artemisinina, rendimento e composição de óleo essencial influenciados por diferentes eliciadores e níveis de adubação NPKPaladini, Marcos Vily 27 February 2012 (has links)
CAPES, CNPq, Fundação Araucária / Artemisia annua L. é uma planta herbácea, anual, originária da China e aclimatada ao Brasil, que produz artemisinina, uma lactona sesquiterpênica utilizada no tratamento da malária. A espécie é a única fonte economicamente viável dessa molécula. Também, é uma espécie altamente aromática e produz grande quantidade de óleo essencial, rico em terpenos. Este trabalho tem como objetivo determinar a influência de moléculas eliciadoras e de níveis de adubação NPK na produção de biomassa, artemisinina e composição do óleo essencial na variedade Artemis de A. annua, produzida em campo na cidade de Pato Branco-PR. Um experimento com adubação foi conduzido em campo durante os anos de 2008 e 2009, onde plantas de A. annua foram submetidas a níveis crescentes de adubação química NPK em um solo de média fertilidade. A partir da dose padrão de adubação (N: 160 kg ha-1; P2O5: 175 Kg ha-1; K2O: 90 Kg ha-1) foram definidos os tratamentos meia dose, uma dose e duas doses, além do tratamento controle, nas formulações Uréia, Super Fosfato Simples e Cloreto de Potássio. Outro experimento com eliciação foi conduzido, onde plantas de A. annua foram submetidas a eliciação com acibenzolar-S-metílico e dois produtos a base de proteína harpina, por meio de três pulverizações semanais, desde o início do período de indução floral até uma semana antes da colheita. Em ambos os experimentos, o material foi seco e separado, a quantificação de artemisinina foi realizada por cromatografia em camada delegada com detecção por densitometria. O perfil químico do óleo foi determinado por cromatografia a gás. No experimento com adubação as massas secas de caule, parte aérea e relação folha caule tiveram ajuste para equação linear, com os melhores resultados para o tratamento duas vezes a dose: 10,43 t ha-1, 14,21 t ha-1, respectivamente para massas secas de caule e parte aérea, e maior relação folha/caule (0,4) para tratamento testemunha. A variável massa seca de folhas obteve ajuste para equação de segundo grau, com máxima eficiência técnica em 1,57 doses e rendimento estimado de 3,87 t ha-1. A influência das doses de adubação NPK sobre teor de artemisinina (média 5,98 kg t-1) e produtividade de
artemisinina (média 19,45 kg ha-1) não apresentou ajustes significativos para reta. Foram identificados 28 componentes no perfil químico óleo essencial que compreendem 94,96% do óleo essencial. As substâncias majoritárias foram cânfora (44,75%), 1,8 cineol (7,90%), γ-muuroleno (6,75%), trans-β-farneseno (6,51%) e mirceno (5,74%). Sete componentes do óleo essencial apresentaram variação em função dos níveis de adubação NPK: p-cimeno, canfeno, trans-β-terpineol, α-pineno, viridifloreno, acetato de mirtenila e β-pineno. O conteúdo relativo desses componentes variou de 0,53 a 2,23%, representando aproximadamente 8% do perfil do óleo essencial. A classe predominante foi monoterpenos (72%). No experimento com eliciação, os eliciadores acibenzolar-S-metílico e proteína harpina não resultaram em alterações significativas nas biomassas de folhas, caule, parte aérea e na relação folha/caule de A. annua; como também não apresentaram diferenças nos teores e rendimento de artemisinina e óleo essencial, No perfil químico foram identificados 31 componentes, que compreendem 91,5% do óleo essencial. Os tratamentos com os eliciadores acibenzilar-S-metílico e harpina não resultaram em diferenças significativas para nenhuma das substâncias identificadas e quantificadas. Os componentes majoritários foram cânfora (43,38%), 1,8 cineol (9,28%), mirceno (7,69%) γ-muuroleno (5,00%), canfeno (4,54%) e trans-β-farneseno (3,98%). Os monoterpenos foram a classe predominante no óleo essencial (79,8%). / Artemisia annua L. is an herbaceous annual plant, originally from China and acclimatized to Brazil, which produces artemisinin, a sesquiterpene lactone used in the treatment of malaria. The species is the only economically viable source of this molecule. Also, it is a highly aromatical species and it produces great amount of essential oil, rich in terpenes. This work has as objective to determine the influence of elicitor molecules and levels of NPK fertilizer in the biomass production, artemisinina and composition of the essential oil in the variety of Artemis A. annua, produced in the field in the town of Pato Branco. An experiment with fertilization was conducted in the field during the years of 2008 and 2009, where plants of A. annua were submitted to increasing levels of NPK chemical fertilizer in a ground of average fertility. From the standard dose of fertilizer (N: 160 kg ha-1; P2O5: 175 kg ha-1; K2O: 90 kg ha-1) it was defined the half dose treatments, one dose and two doses, beyond the control treatment, in the formulations Urea, Super Simple Phosphate and Potassium Chloride. Another experiment with eliciation was lead, where plants of A. annua were submitted to the elciation with acibenzolar-S-methylic and two products harpin-protein based, by means of three weekly sprayings, since the beginning of the floral induction period up to one week before the harvest. In both experiments, the material was dried and separated, the quantification of artemisinin was carried through by thin layer chromatography with detection by densitometry. The chemical profile of the oil was determined by gas chromatography. In the fertilization experiment the dry masses of stalk, aerial part and the relation stalk-leaf had an adjustment for a linear equation, with the best results for the treatment two times the dose: 10,43 t ha-1, 14.21 t ha-1, respectively for dry masses of stalk and aerial part, and greater relation stalk-leaf (0,4) for test treatment. The variable leaf dry mass got an adjustment for second degree equation, with maximum efficiency technique in 1,57 doses and estimated yeld of 3,87 t ha-1. The influence of NPK fertilizer doses on the artemisinin content (average 5,98 kg t-1) and the artemisinin productivity (average 19,45 kg ha-1) did not present significant adjustments for straight line. Twenty-eight
components were identified in the essential oil chemical profile that comprise 94.96%. The majoritarian substances were camphor (44.75%), 1,8 cineole (7.90%), γ-muurolene (6.75%), trans-β-farnesene (6.51%), mircene (5.74%). Seven components of the essential oil showed variation in function of NPK fertilizer levels: p-cymene, camphene, trans-β-terpineol, α-pinene, viridifloreno, acetate of mirtenila and β-pinene, the relative content of these components varied from 0,53 to 2.23% representing about 8% of the essential oil profile. The predominant class was of monoterpenes (72%). In the experiment with eliciation, the elicitors acibenzolar-S-methylic and harpin protein did not result in significant alterations in the leaf, stalk, aerial part biomasses and in the relation stalk-leaf of A. annua; as well as they did not show differences in the artemisinin and essential oil contents and yeld. In the chemical profile 31 components were identified, which comprise 91.5% of the essential oil. The treatments with the elicitors acibenzilar-S-methylic and harpin did not result in significant differences for any of the identified and quantified substances. The majoritarian components were camphor (43.38%), 1,8 cineole (9.28%), mircene (7.69%) γ-muurolene (5.00%), camphene (4.54%) trans-β-farnesene (3.98%). Monoterpenes were the predominant class in the essential oil (79.8%).
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The synthesis and properties of new potentially chemotheraputic [sic] pteridine derivativesParish, Walter Wesley 01 June 1970 (has links)
A new general synthetic method for the preparation of 6-thiopteridines has been developed. The method involves the addition of thiols to intermediate pyrimidine nitrones formed in situ by the reaction of 4-amino-5-nitrosopyrimidines with pyridinium-activated acetonitriles, acetates, acetophenones, and other methylketones. Ca. forty new pteridines were prepared by this method. The preparation of six new 6-pteridinyl ketones, two new 6- pteridinyl ketone thiosemicarbazones, and two new 6-sulfonylpteridines and their 4-acetamido derivatives is also reported. 4-Acetamido-2- amino-7-phenylpteridine 5-oxide was prepared by the reaction of 2- amino-4,6-diacetamido-5-nitrosopyrimidine with either phenylsulfonyl-acetophenone or phenacylpyridinium bromide. Evidence relating to the structure of the acylated 4-amino-5- nitrosopyrimidines used as intermediates in the aforementioned reactions is presented and discussed. Also included in the dissertation are detailed reviews of the following subjects: Pteridine antimalarials, 6-thiopteridines, 6- pteridinesulfonic acids, 6-pteridinesulfonamides, 6-pteridinyl ketones, and pteridine N-oxides.
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Structure-based inhibitor design and validation : application to Plasmodium falciparum glutathione S-transferaseBotha, Maria Magdalena. January 2007 (has links)
Thesis (M.Sc.)(Bioinformatics))-University of Pretoria, 2007. / Summary in English. Includes bibliographical references. Available on the Internet via the World Wide Web.
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Structural model and properties of AdoMetDc domain of the bifunctional Plasmodium falciparum S-adenosylmethionine decarboxylase/Ornithine decarboxylaseWells, Gordon Andreas January 2004 (has links)
Please read the abstract in the section 00front of this document / Dissertation (MSc(Biochemistry))--University of Pretoria, 2004. / Biochemistry / unrestricted
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