7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. doi: 10.1016/j.bmcl.2009.06.042.
David A Sandham  1 ,  Claire Adcock ,  Kamlesh Bala ,  Lucy Barker ,  Zarin Brown ,  Gerald Dubois ,  David Budd ,  Brian Cox ,  Robin A Fairhurst ,  Markus Furegati ,  Catherine Leblanc ,  Jodie Manini ,  Rachael Profit ,  John Reilly ,  Rowan Stringer ,  Alfred Schmidt ,  Katharine L Turner ,  Simon J Watson ,  Jennifer Willis ,  Gareth Williams ,  Caroline Wilson
Affiliations
  • 1. Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Horsham, West Sussex RH12 5AB, United Kingdom. [email protected]
PMID: 19592244 DOI: 10.1016/j.bmcl.2009.06.042
Abstract

High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.