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 | |
| Publication status | Published - May 15 2006 |
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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 journal › Article
}
TY - JOUR
T1 - Antimalarial effect of bis-pyridinium salts, N,N′-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide)
AU - Fujimoto, Kanji
AU - Morisaki, Daiki
AU - Yoshida, Munehiro
AU - Namba, Tetsuto
AU - Kim, Hye-Sook
AU - Wataya, Yusuke
AU - Kourai, Hiroki
AU - Kakuta, Hiroki
AU - Sasaki, Kenji
PY - 2006/5/15
Y1 - 2006/5/15
N2 - 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.
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.
KW - Antimalaria
KW - Bis-pyridinium salt
KW - N,N′-Hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide)
KW - Plasmodium falciparum
KW - QSAR
UR - http://www.scopus.com/inward/record.url?scp=33645891155&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33645891155&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2006.02.030
DO - 10.1016/j.bmcl.2006.02.030
M3 - Article
C2 - 16524728
AN - SCOPUS:33645891155
VL - 16
SP - 2758
EP - 2760
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 10
ER -