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Bioorg Med Chem Lett. 2013 Feb 15;23(4):1022-5. doi: 10.1016/j.bmcl.2012.12.022. Epub 2012 Dec 20.

Novel diaryl ureas with efficacy in a mouse model of malaria.

Author information

1
Department of Medicinal Chemistry, Jacobus Pharmaceutical Company, 37 Cleveland Lane, Princeton, NJ 08540, USA.

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.

PMID:
23313245
PMCID:
PMC3746744
DOI:
10.1016/j.bmcl.2012.12.022
[Indexed for MEDLINE]
Free PMC Article

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