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American Chemical Society, Journal of Medicinal Chemistry, 25(50), p. 6307-6315, 2007

DOI: 10.1021/jm0704752

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Potent antimalarial activity of 2-aminopyridinium salts, amidines, and guanidines

Journal article published in 2007 by Michele Calas, Mahama Ouattara, Mahama Outtara, Giles Piquet, Zyta Ziora, Y. Bordat, Marie-Laure Ancelin ORCID, Roger Escale, Henri Vial
This paper was not found in any repository; the policy of its publisher is unknown or unclear.
This paper was not found in any repository; the policy of its publisher is unknown or unclear.

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Abstract

We describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1 H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10 (-6)-10 (-7) M concentration range. IC 50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC 50