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Entree

Síntese e relação estrutura-atividade de Trypanocidal lignans

Processo: 99/11738-1
Linha de fomento:Bolsas no Brasil - Pós-Doutorado
Vigência (Início): 01 de fevereiro de 2000
Vigência (Término): 30 de abril de 2001
Área do conhecimento:Ciências Exatas e da Terra - Química
Pesquisador responsável:Massuo Jorge Kato
Beneficiário:Kenichi Nihei
Instituição-sede: Instituto de Química (IQ). Universidade de São Paulo (USP). São Paulo , SP, Brasil
Vinculado ao auxílio:98/05074-0 - Conservação e uso sustentável da biodiversidade vegetal do Cerrado e da Mata Atlântica: diversidade química e prospecção de medicamentos potenciais, AP.BTA.TEM
Assunto(s):Doença de Chagas   Trypanosoma cruzi

Resumo

The Chagas' disease is a serious public health problem in the tropics and subtropics of continental America. Treatment by extremely effective drug at the early stage of the disease would lead not only to the alleviation of inflammation in acute stage, but also to the avoidance of dreadful lesion in chronic stage. However, several drugs in use cause severe side effects and are not efficient at the chronic stage. Recently, two highly trypanocidal tetrahydrofuran lignans, (+)-veraguensin and (-)-grandisin have been isolated from Virola surinamesis, a common tree in the Amazon Forest. The major aim in this project is to synthesize several analogs of tetrahydrofuran lignans, specially by means of radical cyclization of cinnamic ester and propargyl alcohol, in which a wide flexibility in the stereochemical control is achievable. Having several analogs, it will be possible to investigate the structure-activity relationship and mode of action on trypanocidal activity. Further improvement in the activity would lead to development of a highly effective therapeutic agent. (AU)