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

Sandham, David A, Adcock, Claire, Bala, Kamlesh, Barker, Lucy, Brown, Zarin, Dubois, Gerald, Budd, David, Cox, Brian, Fairhurst, Robin A, Furegati, Markus, Leblanc, Catherine, Manini, Jodie, Profit, Rachael, Reilly, John, Stringer, Rowan, Schmidt, Alfred, Turner, Katharine L, Watson, Simon J, Willis, Jennifer, Williams, Gareth and Wilson, Caroline (2009) 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 19 (16). pp. 4794-4798. ISSN 0960-894X

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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.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 12 Jan 2015 15:57
Last Modified: 12 Jan 2015 15:57
URI: http://sro.sussex.ac.uk/id/eprint/52052
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