Antimalarial and antiplasmodial activities of norneolignans. Syntheses and SAR.
A systematic change of the substituents and side chain of the norneolignan hinokiresinol afforded a 10 fold improvement of the IC(50) value toward inhibition of the growth of Plasmodium falciparum. The more potent compounds controlled the parasitemia in mice infected with Plasmodium berghei.
Skytte
Dorthe Mondrup
DM
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen Ø, Denmark.
Nielsen
Simon Feldbaek
SF
Chen
Ming
M
Zhai
Lin
L
Olsen
Carl Erik
CE
Christensen
Søren Brøgger
SB
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D066298:In Vitro Techniques; D017705:Lignans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016778:Malaria, Falciparum / Q000188:drug therapy* / Q000469:parasitology; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D013329:Structure-Activity Relationship
D000962:Antimalarials; D017705:Lignans