7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists
journal contribution
posted on 2023-06-08, 19:29authored byDavid 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.