Issue 9, 2012
From the journal:

MedChemComm

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

Bianca Pérez,a   Cátia Teixeira,ab   Inês S. Albuquerque,c   Jiri Gut,d   Philip J. Rosenthal,d   Miguel Prudêncio*c  and  Paula Gomes*a  

* Corresponding authors

a Centro de Investigação em Química da Universidade do Porto, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, R. do Campo Alegre, 687, P-4169-007 Porto, Portugal
E-mail: pgomes@fc.up.pt
Fax: +351 220402659
Tel: +351 220402563

b CICECO, Departamento de Química, Universidade de Aveiro, Campus Universitário de Santiago, 3810-193 Aveiro, Portugal

c Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal
E-mail: mprudencio@fm.ul.pt

d Department of Medicine, San Francisco General Hospital, University of California, San Francisco, CA 94143-0811, USA

Abstract

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.

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

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Article information

DOI
https://doi.org/10.1039/C2MD20113E
Article type
Concise Article
Submitted
02 May 2012
Accepted
16 Jul 2012
First published
19 Jul 2012

Med. Chem. Commun., 2012,3, 1170-1172

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

B. Pérez, C. Teixeira, I. S. Albuquerque, J. Gut, P. J. Rosenthal, M. Prudêncio and P. Gomes, Med. Chem. Commun., 2012, 3, 1170 DOI: 10.1039/C2MD20113E

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