2. Academic Validation
  3. 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists

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

Affiliation

  • 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.

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