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Master's Dissertation
DOI
10.11606/D.9.2017.tde-17102017-154119
Document
Author
Full name
Jeanine Giarolla Vargas
E-mail
Institute/School/College
Knowledge Area
Date of Defense
Published
São Paulo, 2007
Supervisor
Committee
Ferreira, Elizabeth Igne (President)
Chin, Chung Man
Cruz, Maria Luiza
Title in Portuguese
Pró-fármacos dendriméricos de hidroximetilnitrofural potencialmente antichagásicos. Estudo de condições sintéticas para a primeira geração
Keywords in Portuguese
Antiparasitários
Dendrímeros
Doença de Chagas (Quimioterapia)
Latenciação
Planejamento de fármacos
Química farmacêutica
Síntese de fármacos
Abstract in Portuguese
O Trypanosoma cruzi é o agente etiológico da tripanossomíase americana ou doença de Chagas. O vetor desta parasitose é um inseto hemíptero da família Triatominae, conhecido popularmente como barbeiro, chupões, chupança. A doença de Chagas ocorre desde o sul dos EUA até o sul da Argentina e cerca de 20 milhões de pessoas da América Latina correm o risco de adquirir a infecção. O problema desta patologia está na ausência de fármacos não tóxicos e ativos para a fase crônica da doença. O nifurtimox (retirado recentemente do mercado) e benznidazol, utilizados na terapêutica têm alta incidência de efeitos colaterais, o que compromete o tratamento. Face ao exposto, é necessária a pesquisa de novos agentes que sejam eficazes para a cura e bem-estar do paciente chagásico. À vista de tais fatos e utilizando-se o método de modificação molecular latenciação, o objetivo deste trabalho foi o estudo de condições sintéticas para pró-fármacos dendriméricos de hidroximetilnitrofural potencialmente antichagásicos. O hidroximetilnitrofural tem mostrado atividade contra as formas amastigotas e tripomastigotas do Trypanosoma cruzi in vitro. Já os dendrímeros são novas arquiteturas moleculares, estruturas nanoscópicas, extremamente organizadas com massa molecular definida. Possuem diversas vantagens em relação aos polímeros tradicionais e podem atuar como agentes transportadores de fármacos, permitindo-Ihes liberação controlada. Os estudos desenvolvidos acerca das condições reacionais para a obtenção do dendrímero de primeira geração mostraram a dificuldade em se obtê-los. O hidroximetilnitrofural apresentou baixa reatividade nas condições estudadas, o que conduz à necessidade de estudos adicionais sobre novas rotas para a síntese dos dendrímeros a partir dos ésteres desse derivado.
Title in English
Potentially antichagasic dendrimeric prodrugs of hydroxymethylnitrofurazone. Study of synthetic conditions for the first generation
Keywords in English
Antiparasitics
Chagas disease (Chemotherapy)
Dendrimers
Drug planning
Drug synthesis
Latentiation
Pharmaceutical chemistry
Abstract in English
The Trypanosoma cruzi is an etiological agent of American tripanosomiasis or Chagas' disease. The vector of this parasitic disease is a hemipter insect from Triatominae family, known popularly as barber. Chagas' disease occurs from the South of USA to the South of Argentine and about 20 million of people in Latin America are under the risk of acquiring the infection. The problem of this pathology is the absence of non toxic and active drugs for its chronic phase. Nifurtimox (recently removed from the market) and benznidazole, the only that has been available for therapeutics have high incidence of side effects. So, the research of new agents for the cure and welfare of the patient is needed. Taking into account such facts and employing a process of molecular modification, named latentiation, the aim of this work was the study of the synthetic conditions for obtaining potentially antichagasic dendrimeric prodrugs of hydroxymethylnitrofurazone. The hydroxymethylnitrofurazone showed to be active against the trypomastigotes and amastigotes forms of Trypanosoma cruzi in vitro. On the other hand, the dendrimers are new molecular architecture, nanoscopic structure extremely organized with defined molecular weight. They have a wide range of advantages related to traditional polymers and can act as drug carriers, towards drug controlled release. The studies developed concerning the reaction conditions for the attainment of the first generation of dendrimer showed the difficulty in obtaining these prodrugs. The hydroxymethylnitrofurazone presented low reactivity in the studied conditions, which leads to the necessity of developing further studies about new synthetic routes for obtaining dendrimers from its ester derivative.
 
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Publishing Date
2017-10-17
 
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