期刊
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
卷 28, 期 10, 页码 1850-1856出版社
SOC BRASILEIRA QUIMICA
DOI: 10.21577/0103-5053.20170013
关键词
lupeol; terpenoids; 1,2,3-triazole; click chemistry; antiplasmodial activity
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico/CNPq/PRONEX Rede Malaria [555655/2009-1]
- Fundacao de Amparo a Pesquisa do Estado de Minas Gerais/FAPEMIG [CDS APQ 01129-10]
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 mu mol L-1) in relation to lupeol (IC50 117.00 mu mol 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.
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