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Doctoral Thesis
DOI
10.11606/T.9.2016.tde-08112016-162838
Document
Author
Full name
Kátia Cirlene Alves Botelho
E-mail
Institute/School/College
Knowledge Area
Date of Defense
Published
São Paulo, 2008
Supervisor
Committee
Ferreira, Elizabeth Igne (President)
Chin, Chung Man
Marzorati, Liliana
Rando, Daniela Gonçales
Rangel-Yagui, Carlota de Oliveira
Title in Portuguese
Antimaláricos potenciais: latenciação de primaquina e desetilcloroquina e estudo da síntese de pró-fármacos peptídicos de liberação específica
Keywords in Portuguese
Antimaláricos (Síntese química)
Cloroquina
Desetilcloroquina
Latenciação
Malária (Epidemiologia)
Peptídeos
Planejamento de fármacos
Plasmodium (Estudo; Quimioterapia)
Primaquina
Pró-fármaco
Quimioterapia (Aplicações)
Abstract in Portuguese
A Malária continua sendo a mais difundida e devastadora doença infecciosa, com aproximadamente 300 milhões de casos anuais e mais de 2 milhões de pessoas vivendo em áreas de risco. Entre os parasitas do gênero plasmodium causadores da malária em humanos, o plasmodium falciparum é a espécie mais letal. Este projeto teve como objetivo a síntese de pró-fármaco recíproco de cloroquina e primaquina e de pró-fármacos duplicados de cloroquina e de primaquina utilizando, para tanto, espaçantes inespecíficos (carboxílicos). Espera-se que o pró-fármaco recíproco permita a cura radical em casos de malária vivax e que os derivados duplicados apresentem maior eficácia, com diminuição da toxicidade, especialmente no caso do derivado de primaquina. Além desses compostos, propôs-se a síntese de pró-fármacos duplicados de cloroquina mediante a ligação com grupo espaçante específico (peptídeos) à cisão pela falcipaína. Tais derivados são potencialmente ativos em malária causada pelo P. falciparum resistente à cloroquina.
Title in English
Potential antimalarials: Latency of primaquine and desethylchloroquine and study of the synthesis of specific release peptidic prodrugs
Keywords in English
Antimalarials (Chemical synthesis)
Chemotherapy (Applications)
Chloroquine
Desethylchloroquine
Drug planning
Latentization
Malaria (Epidemiology)
Peptides
Plasmodium (Chemotherapy)
Primaquine
Pro-drug
Abstract in English
Malaria remains the world's most widespread and devastating infectious disease, with approximately 300 million annual cases and more than 2 million casualties. Among the protozoan parasites of the genus Plasmodium causing malaria in humans, Plasmodium falciparum is the most lethal species. This project had as objective the synthesis of reciprocal prodrug of chloroqine and primaquine using, for in such a way, inespecífics agents (carboxylics). One expects that the mutual prodrug allows to the radical cure in cases of malaria vivax and that the derivatives duplicates present greater effectiveness, with reduction of the toxicity, especially in the case of the primaquine derivative. Beyond these composites, it was considered synthesis of mutual prodrugs of chloroquine by means of the linking with specific carrier group (peptides) to the split for falcipain. Such derivatives are potentially active in malaria caused for the resistant P. falciparum to the chloroquine.
 
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Publishing Date
2016-11-08
 
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