Synthesis and evaluation of new antimalarial analogues of quinoline alkaloids derived from Cinchona ledgeriana Moens ex Trimen.
In the course of attempts to develop antimalarial drugs, we have designed and synthesized a series of quinoline alkaloide derivatives. Three of them, N-(4-methoxy-3,5-di-tert-butylbenzyl)cinchonidinium bromide (OSL-5), O-benzyl-N-(3,5-di-tert-butyl-4-methoxybenzyl)cinchonidinium bromide (OSL-7), and N-(3,5-di-tert-butyl-4-methoxybenzyl)quininium bromide (OSL-14) show potent activity against Plasmodium falciparum.
Park
Byeoung-Soo
BS
Department of Life Sciences, Soonchunhyang University, Asan-si, 336-600, Chungnam, Republic of Korea.
Kim
Dae-Young
DY
Rosenthal
Philip J
PJ
Huh
Sun-Chul
SC
Lee
Belinda J
BJ
Park
Eun -u
E-
Kim
Sung-Min
SM
Kim
Jang-Eok
JE
Kim
Mi-Hee
MH
Huh
Tae-Lin
TL
Choi
Young-Jae
YJ
Suh
Ki-Hyung
KH
Choi
Won-Sik
WS
Lee
Sung-Eun
SE
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis*; D002738:Chloroquine / Q000494:pharmacology; D002930:Cinchona Alkaloids / Q000138:chemical synthesis*; D015195:Drug Design; D004351:Drug Resistance; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008968:Molecular Conformation; D010961:Plasmodium / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D000962:Antimalarials; D002930:Cinchona Alkaloids; D011804:Quinolines; D002738:Chloroquine