Antimalarial benzo[c]phenanthridines.
Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC(50) below 5ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC(50) below 30ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.
Nyangulu
James M
JM
Department of Pharmaceutical Sciences, University of Strathclyde, 27 Taylor Street, Glasgow, G4 0NR Scotland, UK.
Hargreaves
Samantha L
SL
Sharples
Susan L
SL
Mackay
Simon P
SP
Waigh
Roger D
RD
Duval
Olivier
O
Mberu
Eddie K
EK
Watkins
William M
WM
D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D009429:Netropsin / Q000737:chemistry / Q000494:pharmacology; D010617:Phenanthridines / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000502:physiology
D000962:Antimalarials; D010617:Phenanthridines; C404513:ethoxidine; D009429:Netropsin