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

Research output: Contribution to journalArticle

32 Citations (Scopus)

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 3.5 μM to 10 nM. 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.

Original languageEnglish
Pages (from-to)2758-2760
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number10
DOIs
Publication statusPublished - May 15 2006

Keywords

  • Antimalaria
  • Bis-pyridinium salt
  • N,N′-Hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide)
  • Plasmodium falciparum
  • QSAR

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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