Novel diaryl ureas with efficacy in a mouse model of malaria | Academic Article individual record
abstract

Exploration of triclosan analogs has led to novel diaryl ureas with significant potency against in vitro cultures of drug-resistant and drug-sensitive strains of the human malaria parasite Plasmodium falciparum. Compound 18 demonstrated EC(50) values of 37 and 55 nM versus in vitro cultured parasite strains and promising in vivo efficacy in a Plasmodium berghei antimalarial mouse model, with >50% survival at day 31 post-treatment when administered subcutaneously at 256 mg/kg. This series of compounds provides a chemical scaffold of novel architecture, as validated by cheminformatics analysis, to pursue antimalarial drug discovery efforts.

author list (cited authors)
Anderson, J. W., Sarantakis, D., Terpinski, J., Kumar, T., Tsai, H., Kuo, M., ... Freundlich, J. S.
publication date
2013
publisher
Elsevier BV Publisher
keywords
  • Diaryl Urea
  • Plasmodium Falciparum
  • Malaria
  • Drug Discovery
altmetric score

9.756

citation count

13