PRIMACINS, N-cinnamoyl-primaquine conjugates, with improved liver-stage antimalarial activity


Novel primaquine derivatives, obtained by conjugation of the drug's aliphatic amine with different cinnamic acids, resulted in increased in vitro activity, compared to primaquine, against liver-stage malarial parasites. The compounds were non-cytotoxic to human hepatoma cells, suggesting that they are a promising new class of agents for the treatment and prevention of malaria.




Biochemistry & Molecular Biology; Pharmacology & Pharmacy


Perez, B; Teixeira, C; Albuquerque, IS; Gut, J; Rosenthal, PJ; Prudencio, M; Gomes, P

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This work was mainly supported by Fundacao para a Ciencia e a Tecnologia (FCT, Portugal) through project PTDC/QUI-QUI/116864/2010. Funding to CIQUP through the strategic project PEst-C/QUI/UI0081/2011 is also acknowledged to FCT. CT thanks FCT for post-doctoral grant SFRH/BPD/62967/2009. MP acknowledges FCT for grant PTDC/SAU-MII/099118/2008. ISA is hired under FCT grant PTDC/SAU-GMG/100313/2008. Thanks are due to FCT also for both the LC-MS and NMR facilities, respectively funded through projects CONC-REEQ/275/QUI and REDE/1517/RMN/2005. Antonio M. Mendes is acknowledged for his help with data analysis and presentation.

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