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

Kanji Fujimoto, Daiki Morisaki, Munehiro Yoshida, Tetsuto Namba, Hye-Sook Kim, 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

Fingerprint

Antimalarials
Bromides
Salts
Chain length
Chloroquine
Plasmodium falciparum
Derivatives

Keywords

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

ASJC Scopus subject areas

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

Cite this

Antimalarial effect of bis-pyridinium salts, N,N′-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide). / Fujimoto, Kanji; Morisaki, Daiki; Yoshida, Munehiro; Namba, Tetsuto; Kim, Hye-Sook; Wataya, Yusuke; Kourai, Hiroki; Kakuta, Hiroki; Sasaki, Kenji.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 10, 15.05.2006, p. 2758-2760.

Research output: Contribution to journalArticle

Fujimoto, Kanji ; Morisaki, Daiki ; Yoshida, Munehiro ; Namba, Tetsuto ; Kim, Hye-Sook ; Wataya, Yusuke ; Kourai, Hiroki ; Kakuta, Hiroki ; Sasaki, Kenji. / Antimalarial effect of bis-pyridinium salts, N,N′-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide). In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 10. pp. 2758-2760.
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AU - Namba, Tetsuto

AU - Kim, Hye-Sook

AU - Wataya, Yusuke

AU - Kourai, Hiroki

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