4-amino bis-pyridinium derivatives as novel antileishmanial agents.

ABSTRACT: The antileishmanial activity of a series of bis-pyridinium derivatives that are analogues of pentamidine have been investigated, and all compounds assayed were found to display activity against promastigotes and intracellular amastigotes of Leishmania donovani and Leishmania major, with 50% effective concentrations (EC50s) lower than 1 μM in most cases. The majority of compounds showed similar behavior in both Leishmania species, being slightly more active against L. major amastigotes. However, compound VGP-106 {1,1'-(biphenyl-4,4'-diylmethylene)bis[4-(4-bromo-N-methylanilino)pyridinium] dibromide} exhibited significantly higher activity against L. donovani amastigotes (EC50, 0.86 ± 0.46 μM) with a lower toxicity in THP-1 cells (EC50, 206.54 ± 9.89 μM). As such, VGP-106 was chosen as a rep

SUBMITTER: Gomez-Perez V 

PROVIDER: S-EPMC4068582 | biostudies-literature | 2014 Jul

REPOSITORIES: biostudies-literature