Novel imidazoline compounds as partial or full agonists of D₂-like dopamine receptors inspired by I₂-imidazoline binding sites ligand 2-BFI

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• 作者：Gianfabio Giorgioni ; Dario Ambrosini ; Cristian Vesprini ; Alan Hudson ; Cinzia Nasuti ; Antonio Di Stefano ; Piera Sozio ; Osele Ciampi ; Barbara Costa ; Claudia Martini ; Antonio Carrieri ; Giuseppe Carbonara
• 关键词：Dopamine receptors ; 2-BFI ; Imidazoline binding sites ; I2-IBS ; D2-like receptors ; Imidazoline
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：1 October 2010
• 年：2010
• 卷：18
• 期：19
• 页码：7085-7091
• 全文大小：423 K

文摘

Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a–k inspired by 2-BFI scaffold to assess imidazoline molecules as D₂-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided partial (3f) or nearly full (3e and 3h) agonists, all endowed with D₂-like potency comparable to that of dopamine.