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-Like Dopamine Receptors Inspired by I2-Imidazoline Binding Sites Ligand 2-BFI
GIORGIONI, Gianfabio;AMBROSINI, Dario;VESPRINI, Christian;NASUTI, Cinzia Carla;PIGINI, Maria
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.File in questo prodotto:
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