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Title: Synthesis by click reactions and antiplasmodial activity of Lupeol 1,2,3-Triazole derivatives.
Authors: Borgati, Tatiane Freitas
Pereira, Guilherme Rocha
Brandão, Geraldo Célio
Santos, Juliana de Oliveira
Fernandes, Dayane Aparecida Morais
Paula, Renata Cristina de
Nascimento, Maria Fernanda Alves do
Soares, Luciana Ferreira
Lopes, Júlio César Dias
Souza Filho, José Dias de
Oliveira, Alaíde Braga de
Keywords: Terpenoids
Click chemistry
Issue Date: 2017
Citation: BORGATI, T. F. et al. Synthesis by click reactions and antiplasmodial activity of Lupeol 1,2,3-Triazole derivatives. Journal of the Brazilian Chemical Society, v. 00, p. 1-7, 2017. Disponível em: <>. Acesso em: 29 ago. 2017.
Abstract: Lupeol, a triterpene frequently found in Asteraceae plant species, showed moderate to low activity in different strains of Plasmodium falciparum, the most virulent malaria etiological agents. In this work, lupeol was isolated from Parahancornia fasciculata, a plant that is used to treat malaria in the Amazonia region. In the search of more activity lupeol derivatives, five new 1,2,3-triazole hybrid molecules were synthetized by copper-catalyzed azide-alkyne cycloaddition. The antiplasmodial activity of the semi-synthetic compounds were evaluated by the lactate dehydrogenase assay; the lupeol propargyl ether was the only one to disclosing increased activity (half maximal inhibitory concentration-IC50-62.0 ± 1.92 μmol L-1) in relation to lupeol (IC50 117.00 μmol L-1). Therefore, this work revealed a new class of interesting lupeol derivatives that can be obtained by linking electron donors to the hydroxy group at C-3.
ISSN: 1678-4790
metadata.dc.rights.license: Os trabalhos publicados no periódico Journal of the Brazilian Chemical Society, exceto onde identificado, está sob licença Creative Commons que permite copiar, distribuir e transmitir o trabalho em desde que sejam citados o autor e o licenciante. Fonte: Journal of the Brazilian Chemical Society <>. Acesso em: 23 jan. 2020.
Appears in Collections:DEFAR - Artigos publicados em periódicos

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