Synthesis and structure–activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists

Autor:	Laura Caberlotto, Thorsten Genski, Matteo Biagetti, Domenica Antonia Pizzi, Colin Philip Leslie, Laura Zonzini, Jonathan Mark Bentley, Angelica Mazzali, Catia Seri, Romano Di Fabio
Rok vydání:	2010
Předmět:	medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Cell Line Structure-Activity Relationship Drug Discovery medicine Animals Humans Structure–activity relationship Amines Molecular Biology Bicyclic molecule Chemistry Organic Chemistry Antagonist Stereoisomerism Metabolic stability Small molecule Rats Receptors Neuropeptide Y Lipophilicity Molecular Medicine Azabicyclo Compounds
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:4741-4744
ISSN:	0960-894X
Popis:	A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modification of a screening hit. Structure–activity relationships and efforts undertaken to achieve a favourable pharmacokinetic profile in rat are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e286dbfa8e57e9fa4a0f617b2fc278d https://doi.org/10.1016/j.bmcl.2010.06.140 Zobrazit plný text záznamu Full Text from ScienceDirect