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dc.contributor.authorSoares, Breno Almeida
dc.date.accessioned2023-12-22T03:04:05Z-
dc.date.available2023-12-22T03:04:05Z-
dc.date.issued2009-09-25
dc.identifier.citationSOARES, Breno Almeida. Sintese e avaliação de atividade tripanocida de novos heterociclos da classe dos 1,2,4-OXADIAZÓIS, derivados e análogos da amida natural piperina.. 2009. 183 f. Dissertação (Mestrado em Química). Instituto de Ciências Exatas, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ, 2009.por
dc.identifier.urihttps://rima.ufrrj.br/jspui/handle/20.500.14407/14655-
dc.description.abstractEste trabalho se insere numa linha de pesquisa que visa a utilização de produtos naturais abundantes e accessíveis na síntese de novas moléculas com potencial atividade anti-chagásica. Estudos recentes em nosso laboratório demonstraram a atividade antiparasitária da piperina e de uma série de derivados e análogos sobre o Trypanosoma cruzi, agente etiológico da doença de Chagas. Utilizando o bioisosterismo como estratégia de modificação molecular, descrevemos aqui o planejamento, a síntese e a avaliação antiparasitária de derivados da classe dos 1,2,4-oxadiazóis. A etapa-chave da estratégia sintética utilizada envolveu a reação de SNAC da benzamidoxima com cloretos de ácidos, seguida de ciclização, que permitiu a preparação de oito novos 1,2,4- oxadiazóis. A avaliação da atividade tóxica destes novos derivados contra a forma epimastigota do T. cruzi confirmou a relação bioisostérica entre a amida natural e os novos derivados preparados, evidenciando o oxadiazol 55 derivado direto da piperina, como o composto mais ativo da série.por
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior, CAPES, Brasil.por
dc.formatapplication/pdf*
dc.languageporpor
dc.publisherUniversidade Federal Rural do Rio de Janeiropor
dc.rightsAcesso Abertopor
dc.subjectOrganic Synthesiseng
dc.subjectTrypanosomeeng
dc.subjectAmideeng
dc.subjectAntiparasiticseng
dc.subjectSintese Orgânicapor
dc.subjectTripanossomopor
dc.subjectAmidapor
dc.subjectAntiparasitáriospor
dc.titleSintese e avaliação de atividade tripanocida de novos heterociclos da classe dos 1,2,4-OXADIAZÓIS, derivados e análogos da amida natural piperinapor
dc.title.alternativeSYNTHESIS AND EVALUATION OF TRIPANOCIDAL ACTIVITY OF NEW HETEROCYCLES OF THE 1,2,4-OXADIAZIAL CLASS, DERIVATIVES AND ANALOGS OF THE NATURAL AMID PIPERINAeng
dc.typeDissertaçãopor
dc.description.abstractOtherThis work is part of a research project which investigates the utilization of abundant and accessible natural products in the synthesis of new molecules with potential activity against Chagas´ disease. Recent studies carried out in our laboratory showed activity against Trypanosoma cruzi for piperine, a major component of Piper nigrum and for a series of its derivatives and analogues. Using bioisosterism as a strategy for molecular modification, we describe here the design, synthesis and antiparasitic evaluation of class of derivatives of 1,2,4-oxadiazole. The key step of the synthetic strategy used involved the SNAC reaction of the benzamidoxima with acid chlorides followed by cyclization, which allowed the preparation of eight new 1,2,4-oxadiazole The evaluation of the toxic activity of these new derivatives against epimastigote form of T. cruzi confirmed the bioisosteric relationship between the natural amide and the new products prepared, showing the oxadiazole 55 direct derived from piperine, as the most active compound in the series.eng
dc.contributor.advisor1Lima, Marco Edilson Freire de
dc.contributor.advisor1ID880.202.667-04por
dc.contributor.advisor1Latteshttp://lattes.cnpq.br/8392420706762318por
dc.contributor.referee1Lima, Lidia Moreira
dc.contributor.referee2Ferreira, Aurélio Baird Buarque
dc.contributor.referee3Pinheiro, Sérgio
dc.creator.ID098.867.667-27por
dc.creator.Latteshttp://lattes.cnpq.br/0117694345431491por
dc.publisher.countryBrasilpor
dc.publisher.departmentInstituto de Ciências Exataspor
dc.publisher.initialsUFRRJpor
dc.publisher.programPrograma de Pós-Graduação em Químicapor
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