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 › peer-review

33 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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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 › peer-review

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

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.",

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

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

note = "Funding Information: This work was supported by Grant-in-Aid for Scientific Research (C) (No. 17590088) from the Ministry of Education, Sciences, Sports and Culture of Japan.",

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AU - Fujimoto, Kanji

AU - Morisaki, Daiki

AU - Yoshida, Munehiro

AU - Namba, Tetsuto

AU - Hye-Sook, Kim

AU - Wataya, Yusuke

AU - Kourai, Hiroki

AU - Kakuta, Hiroki

AU - Sasaki, Kenji

N1 - Funding Information: This work was supported by Grant-in-Aid for Scientific Research (C) (No. 17590088) from the Ministry of Education, Sciences, Sports and Culture of Japan.

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AB - 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.

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KW - Plasmodium falciparum

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