Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds

Author(s):Show less -

Passalacqua, Thais Gaban ^{[1, 2]} ; Dutra, Luiz Antonio ^{[3, 4]} ; de Almeida, Leticia ^{[1, 2]} ; Arenas Velasquez, Angela Maria ^{[1, 2]} ; Esteves Torres, Fabio Aurelio ^{[1, 2]} ; Yamasaki, Paulo Renato ^[3] ; dos Santos, Mariana Bastos ^[5] ; Regasini, Luis Octavio ^[5] ; Michels, Paul A. M. ^[6] ; Bolzani, Vanderlan da Silva ^[1] ; Graminha, Marcia A. S. ^{[3, 2]}

Affiliation

^[1] UNESP, Inst Quim, BR-14800060 Araraquara, SP - Brazil

^[2] Programa Posgrad Biotecnol, Florianopolis, SC - Brazil

^[3] Univ Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil

^[4] Programa Pos Grad Ciencias Farmaceut, Florianopolis, SC - Brazil

^[5] Univ Estadual Paulista, Inst Biociencias Letras & Ciencias Exatas, BR-15054000 Sao Jose Do Rio Preto, SP - Brazil

^[6] Univ Edinburgh, Inst Struct & Mol Biol, Edinburgh EH8 9YL, Midlothian - Scotland

• Document type: Journal article
• Source: Bioorganic & Medicinal Chemistry Letters; v. 25, n. 16, p. 3342-3345, AUG 15 2015.
• Web of Science Citations: 28

Abstract

Chalcones form a class of compounds that belong to the flavonoid family and are widely distributed in plants. Their simple structure and the ease of preparation make chalcones attractive scaffolds for the synthesis of a large number of derivatives enabling the evaluation of the effects of different functional groups on biological activities. In this Letter, we report the successful synthesis of a series of novel prenylated chalcones via Claisen-Schmidt condensation and the evaluation of their effect on the viability of the Trypanosomatidae parasites Leishmania amazonensis, Leishmania infantum and Trypanosoma cruzi. (C) 2015 Elsevier Ltd. All rights reserved. (AU)

• FAPESP's process: 10/16732-2 - Searching for new antigens for canine visceral leishmaniasis serodiagnostic methods improvement: study of Lc06, Lc22, Lc24 and Lc36 genes
• Grantee: Marcia Aparecida Silva Graminha
• Support Opportunities: Regular Research Grants