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)

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

Research output: Contribution to journal › Article

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 language	English
Pages (from-to)	2758-2760
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2006.02.030
Publication status	Published - 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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Fujimoto, K., Morisaki, D., Yoshida, M., Namba, T., Hye-Sook, K., Wataya, Y., Kourai, H., Kakuta, H., & Sasaki, K. (2006). Antimalarial effect of bis-pyridinium salts, N,N′-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide). Bioorganic and Medicinal Chemistry Letters, 16(10), 2758-2760. https://doi.org/10.1016/j.bmcl.2006.02.030

Antimalarial effect of bis-pyridinium salts, N,N′-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide). / Fujimoto, Kanji; Morisaki, Daiki; Yoshida, Munehiro; Namba, Tetsuto; Hye-Sook, Kim; 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 journal › Article

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AU - Namba, Tetsuto

AU - Hye-Sook, Kim

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