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.

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

DI STEFANO, Antonio;SOZIO, Piera;
2010-01-01

Abstract

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11564/173395
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