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

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.

authors

• Sacchettini, James

published proceedings

• Bioorg Med Chem Lett

altmetric score

• 9.006

author list (cited authors)

• Anderson, J. W., Sarantakis, D., Terpinski, J., Kumar, T., Tsai, H., Kuo, M., ... Freundlich, J. S.

citation count

• 20

complete list of authors

• Anderson, John W||Sarantakis, Dimitri||Terpinski, Jacek||Kumar, TR Santha||Tsai, Han-Chun||Kuo, Mack||Ager, Arba L||Jacobs, William R||Schiehser, Guy A||Ekins, Sean||Sacchettini, James C||Jacobus, David P||Fidock, David A||Freundlich, Joel S

publication date

• February 2013

publisher

• Elsevier  Publisher

published in

• Bioorganic and Medicinal Chemistry Letters  Journal

keywords

• Animals
• Antimalarials
• Benzene Derivatives
• Disease Models, Animal
• Drug Discovery
• Malaria, Falciparum
• Mice
• Urea

PubMed Central ID

• 23313245

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2012.12.022

start page

• 1022

end page

• 1025

volume

• 23

issue

• 4

URL

• http://dx.doi.org/10.1016/j.bmcl.2012.12.022