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

Autor:	Jodie Manini, Claire Adcock, Alfred Schmidt, Zarin Brown, Robin Alec Fairhurst, Rachael Profit, John Reilly, David C. Budd, Caroline Wilson, Simon J. Watson, Brian Cox, Kamlesh Bala, Jennifer Willis, Lucy Barker, Markus Furegati, David Andrew Sandham, Katharine L. Turner, Rowan Stringer, Catherine Leblanc, Gareth Williams, Gerald Dubois
Rok vydání:	2009
Předmět:	medicine.drug_class Pyridines Clinical Biochemistry Receptors Prostaglandin Anti-Inflammatory Agents Pharmaceutical Science Administration Oral Acetates Biochemistry Permeability Acetic acid chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Potency Animals Humans Receptors Immunologic Receptor Molecular Biology Whole blood Organic Chemistry Antagonist Receptor antagonist Bioavailability Rats Eosinophils chemistry Microsomes Liver Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 19(16)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::662232891c4a20f4a3460f90d84eb7a6 https://pubmed.ncbi.nlm.nih.gov/19592244 Zobrazit plný text záznamu Full Text from ScienceDirect