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 .

Perspectives

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.

Read Publication

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

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