Journal
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Volume 57, Issue 10, Pages 5112-5115Publisher
AMER SOC MICROBIOLOGY
DOI: 10.1128/AAC.00557-13
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Funding
- FEDER funds through Programa Operacional Factores de Competitividade-COMPETE [FCOMP-01-0124-FEDER-020963]
- Portuguese National funds through Fundacao para a Ciencia e a Tecnologia [PTDC/QUI-QUI/116864/2010]
- Universidade do Porto [PP-IJUP2011-64]
- FCT [Pest-C/QUI/UI0081/2011, SFRH/BPD/62967/2009, SFRH/BD/36661/2007, SFRH/BD/86166/2012]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/86166/2012, SFRH/BD/36661/2007] Funding Source: FCT
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A series of cinnamic acid conjugates of primaquine and chloroquine were evaluated for their in vitro antileishmanial activities. Although primaquine derivatives had modest activity, chloroquine conjugates exhibited potent activity against both promastigotes (50% inhibitory concentration [IC50] = 2.6 to 21.8 mu M) and intramacrophagic amastigotes (IC50 = 1.2 to 9.3 mu M) of Leishmania infantum. Both the high activity of these chloroquine analogues and their mild-to-low toxicity toward host cells make them promising leads for the discovery of new antileishmanial agents.
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