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

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• 作者：Kanji Fujimoto ; Daiki Morisaki ; Munehiro Yoshida ; Tetsuto Namba ; Kim Hye-Sook ; Yusuke Wataya ; Hiroki Kourai ; Hiroki Kakuta and Kenji Sasaki
• 关键词：Antimalaria ; Bis-pyridinium salt ; N ; N′ ; -Hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide) ; Plasmodium falciparum ; QSAR
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 May 2006
• 年：2006
• 卷：16
• 期：10
• 页码：2758-2760
• 全文大小：101 K

文摘

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.