WR 146459 is an orally active 9-phenanthrenecarbinol and antimalarial agent. WR 146459 bears a 2-piperidyl substituent on its 9-carbinol moiety. WR 146459 inhibits hypoxanthine uptake by Plasmodium falciparum strains, reducing parasite viability. WR 146459 can be used for the research of malaria [1].
In Vivo, WR 146459 (20-640 mg/kg; p.o.; single administration three days post-infection) exhibits oral antimalarial activity in Plasmodium berghei-infected ICR/HA Swiss mice with a CD50 of 533 mg/kg[1].
In Vitro, WR 146459 (13.55-135.5 ng/mL) potently inhibits growth of Chloroquine -sensitive Plasmodium falciparum (Camp strain) with an ID50 of 2.14 ng/mL and Chloroquine-resistant Plasmodium falciparum (Smith strain) with an ID50 of 1.41 ng/mL in hypoxanthine uptake assay[1].
References:
[1]. Childs GE, et al. Comparison of in vitro and in vivo antimalarial activities of 9-phenanthrenecarbinols. Ann Trop Med Parasitol. 1984 Feb;78(1):13-20.
In Vivo, WR 146459 (20-640 mg/kg; p.o.; single administration three days post-infection) exhibits oral antimalarial activity in Plasmodium berghei-infected ICR/HA Swiss mice with a CD50 of 533 mg/kg[1].
In Vitro, WR 146459 (13.55-135.5 ng/mL) potently inhibits growth of Chloroquine -sensitive Plasmodium falciparum (Camp strain) with an ID50 of 2.14 ng/mL and Chloroquine-resistant Plasmodium falciparum (Smith strain) with an ID50 of 1.41 ng/mL in hypoxanthine uptake assay[1].
References:
[1]. Childs GE, et al. Comparison of in vitro and in vivo antimalarial activities of 9-phenanthrenecarbinols. Ann Trop Med Parasitol. 1984 Feb;78(1):13-20.