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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

✍ Scribed by Matteo Biagetti; Colin Philip Leslie; Angelica Mazzali; Catia Seri; Domenica Antonia Pizzi; Jonathan Bentley; Thorsten Genski; Romano Di Fabio; Laura Zonzini; Laura Caberlotto

Book ID: 104004605
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 256 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.06.140

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✦ Synopsis

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.

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