title: 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
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.
authors: Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Horsham, West Sussex RH12 5AB, United Kingdom. david.sandham@novartis.com
authors: David A
authors: DA
authors: Sandham
authors: Claire
authors: C
authors: Adcock
authors: Kamlesh
authors: K
authors: Bala
authors: Lucy
authors: L
authors: Barker
authors: Zarin
authors: Z
authors: Brown
authors: Gerald
authors: G
authors: Dubois
authors: David
authors: D
authors: Budd
authors: Brian
authors: B
authors: Cox
authors: Robin A
authors: RA
authors: Fairhurst
authors: Markus
authors: M
authors: Furegati
authors: Catherine
authors: C
authors: Leblanc
authors: Jodie
authors: J
authors: Manini
authors: Rachael
authors: R
authors: Profit
authors: John
authors: J
authors: Reilly
authors: Rowan
authors: R
authors: Stringer
authors: Alfred
authors: A
authors: Schmidt
authors: Katharine L
authors: KL
authors: Turner
authors: Simon J
authors: SJ
authors: Watson
authors: Jennifer
authors: J
authors: Willis
authors: Gareth
authors: G
authors: Williams
authors: Caroline
authors: C
authors: Wilson
mesh_terms: D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D004804:Eosinophils / Q000187:drug effects / Q000276:immunology; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D010539:Permeability; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C413877:1H-pyrrolo(2,3-b)pyridine-3-acetic acid; D000085:Acetates; D000893:Anti-Inflammatory Agents; D011725:Pyridines; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor