Antimalarial effect of bis-pyridinium salts, N,N'-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide)

  • Bioorg Med Chem Lett. 2006 May 15;16(10):2758-60. doi: 10.1016/j.bmcl.2006.02.030.
Kanji Fujimoto  1 ,  Daiki Morisaki ,  Munehiro Yoshida ,  Tetsuto Namba ,  Kim Hye-Sook ,  Yusuke Wataya ,  Hiroki Kourai ,  Hiroki Kakuta ,  Kenji Sasaki
Affiliations
  • 1. Okayama University, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 1-1-1 Tsushima-Naka, Okayama 700-8530, Japan.
PMID: 16524728 DOI: 10.1016/j.bmcl.2006.02.030
Abstract

The in vitro antimalarial activity of bis-pyridinium salts, N,N'-hexamethylenebis(4-carbamoyl-1-decylpyridinium bromide) and their derivatives, against the Plasmodium falciparum FCR-3 strain (ATCC 30932, chloroquine-sensitive) was evaluated. All test compounds exhibited antimalarial activity over a concentration range of 3.5microM to 10nM. The chain length of the N1-alkyl moiety was found to be very beneficial in terms of antimalarial activity, and in this series of compounds, the most appropriate N1-alkyl chain length was found to be eight.