The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor

Autor:	Andrea Colombo, Izzy Boyfield, Christopher N. Johnson, Alessandra Consonni, Emma M. Jarvie, Victoria J. Bolton, Darren Jason Mitchell, Paolo Celestini, Michael A. Briggs, Sharon C Stratton, James Myatt, Geoffrey Stemp, David MacPherson, Alexander J. Stevens, Jon T. Seal, Stefania Gagliardi, Steven J. Stanway, Macdonald Gregor James, Mauro Riccaboni, Kate Lapsley, Susan Marie Westaway, Silvano Ronzoni, Gareth J. Sanger, Tom D. Heightman, Kim L. Matthews, Samantha Louisa Brown, Mervyn Thompson, Elizabeth Conway
Rok vydání:	2008
Předmět:	Agonist Receptors Neuropeptide medicine.drug_class Stereochemistry Pyridines Motilin receptor Chemistry Pharmaceutical Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Motilin Receptors Gastrointestinal Hormone Inhibitory Concentration 50 In vivo Drug Discovery Gastrins medicine Animals Humans Molecular Biology ADME G protein-coupled receptor Chemistry digestive oral and skin physiology Organic Chemistry Small molecule Carbon Rats Kinetics Models Chemical Drug Design Molecular Medicine Rabbits
Zdroj:	Bioorganicmedicinal chemistry letters. 18(24)
ISSN:	1464-3405
Popis:	Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and ADME profiles. Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel small molecule motilin receptor agonist for further evaluation as a gastroprokinetic agent.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2cf8a53bdb66c538b47ff91cc8129e4 https://pubmed.ncbi.nlm.nih.gov/19006669 Zobrazit plný text záznamu Full Text from ScienceDirect