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

Kanji Fujimoto; Daiki Morisaki; Munehiro Yoshida; Tetsuto Namba; Kim Hye-Sook; Yusuke Wataya; Hiroki Kourai; Hiroki Kakuta; Kenji Sasaki

doi:10.1016/j.bmcl.2006.02.030

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. Epub 2006 Mar 9.

Authors

Kanji Fujimoto¹, Daiki Morisaki, Munehiro Yoshida, Tetsuto Namba, Kim Hye-Sook, Yusuke Wataya, Hiroki Kourai, Hiroki Kakuta, Kenji Sasaki

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antimalarials / chemistry
Antimalarials / pharmacology*
Cell Line, Tumor
Mice
Plasmodium falciparum / drug effects
Pyridinium Compounds / chemistry
Pyridinium Compounds / pharmacology*

Substances

Antimalarials
Pyridinium Compounds