Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity

Autor:	Susan Helen Davis, Gillian A. Bottomley, Chrystelle Marie Rasamison, Phillip Clarke, Eleanor Curtis, James Charles Bell, John Keily, Patrick Eric Hanrahan, Gary Moore, Stuart Bradley, Graham Dawson, Jason Bloxham, James G. Horswill
Rok vydání:	2011
Předmět:	Male medicine.medical_specialty Clinical Biochemistry hERG Pharmaceutical Science Administration Oral Biological Availability Pharmacology Biochemistry Type ii diabetes Rats Sprague-Dawley Structure-Activity Relationship Internal medicine Diabetes mellitus Drug Discovery medicine Structure–activity relationship Potency Animals Humans Hypoglycemic Agents Obesity Receptor Receptors Ghrelin Molecular Biology Quinazolinones Aza Compounds biology Chemistry Organic Chemistry medicine.disease Ether-A-Go-Go Potassium Channels Rats Kinetics Endocrinology Diabetes Mellitus Type 2 Drug Design biology.protein Molecular Medicine Ghrelin Hydrophobic and Hydrophilic Interactions
Zdroj:	Bioorganicmedicinal chemistry letters. 22(6)
ISSN:	1464-3405
Popis:	Substituted azaquinazolinones were identified as antagonists of the GHSr-1A receptor for the treatment of type II diabetes and obesity. Optimisation for potency and LogD lead to the identification of orally bioavailable, potent antagonists with improved selectivity over hERG.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcc4431f48abf7265b60957ceae28bcd https://pubmed.ncbi.nlm.nih.gov/22342626 Zobrazit plný text záznamu Full Text from ScienceDirect