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
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- 作者：Matteo Biagetti ; Colin Philip Leslie ; Angelica Mazzali ; Catia Seri ; Domenica Antonia Pizzi ; Jonathan Bentley ; Thorsten Genski ; Romano Di Fabio ; Laura Zonzini ; Laura Caberlotto
- 关键词：Neuropeptide Y ; NPY Y5 ; Antagonists
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 August 2010
- 年：2010
- 卷：20
- 期：16
- 页码：4741-4744
- 全文大小：256 K
文摘
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.