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

journal contribution
posted on 2023-06-08, 19:29 authored by David A Sandham, 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
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.

History

Publication status

  • Published

Journal

Bioorganic and Medicinal Chemistry Letters

ISSN

0960-894X

Publisher

Elsevier

Issue

16

Volume

19

Page range

4794-4798

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-12

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