Novel diaryl ureas with efficacy in a mouse model of malaria

  • John W. Anderson, Dimitri Sarantakis, Jacek Terpinski, T.R. Santha Kumar, Han-Chun Tsai, Mack Kuo, Arba L. Ager, William R. Jacobs Jr., Guy A. Schiehser, Sean Ekins, James C. Sacchettini, David P. Jacobus, David A. Fidock, Joel S. Freundlich
  • Bioorganic & Medicinal Chemistry Letters, February 2013, Elsevier
  • DOI: 10.1016/j.bmcl.2012.12.022

What is it about?

Starting from triclosan led to the development of diaryl ureas. These compounds had nM activity in vitro and in vivo activity against P. Berghei. A pharmacophore was generated with 34 compounds that pulled out compoundsin the GSK library of antimalarials.

Why is it important?

A novel class of compounds was described with in vivo activity. The pharmacophore could be used to identify novel compounds for testing in future .


Dr Sean Ekins
Collaborations in Chemistry

My role in this work was the pharmacophore and database search. Potential to use similar approaches to other classes of compounds.

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The following have contributed to this page: Dr Sean Ekins, Joel Freundlich, and Professor David A Fidock