Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5294-8. doi: 10.1016/j.bmcl.2008.08.043.
Nathalie Bouloc  1 ,  Jonathan M Large ,  Ela Smiljanic ,  David Whalley ,  Keith H Ansell ,  Christopher D Edlin ,  Justin S Bryans
Affiliations
  • 1. Drug Discovery Group, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, UK.
PMID: 18774709 DOI: 10.1016/j.bmcl.2008.08.043
Abstract

A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.