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 - 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.
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 -