title: Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
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 D(2)-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 D(2)-like potency comparable to that of dopamine.
authors.affiliation: Scuola di Scienze del Farmaco e dei Prodotti della Salute, Università degli Studi di Camerino, via Sant'Agostino 1, 62032 Camerino, Italy. gianfabio.giorgioni@unicam.it
authors.forename: Gianfabio
authors.initials: G
authors.lastname: Giorgioni
authors.forename: Dario
authors.initials: D
authors.lastname: Ambrosini
authors.forename: Cristian
authors.initials: C
authors.lastname: Vesprini
authors.forename: Alan
authors.initials: A
authors.lastname: Hudson
authors.forename: Cinzia
authors.initials: C
authors.lastname: Nasuti
authors.forename: Antonio
authors.initials: A
authors.lastname: Di Stefano
authors.forename: Piera
authors.initials: P
authors.lastname: Sozio
authors.forename: Osele
authors.initials: O
authors.lastname: Ciampi
authors.forename: Barbara
authors.initials: B
authors.lastname: Costa
authors.forename: Claudia
authors.initials: C
authors.lastname: Martini
authors.forename: Antonio
authors.initials: A
authors.lastname: Carrieri
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Carbonara
authors.forename: Christoph
authors.initials: C
authors.lastname: Enzensperger
authors.forename: Maria
authors.initials: M
authors.lastname: Pigini
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D017448:Receptors, Dopamine D2 / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D001572:Benzofurans; D007093:Imidazoles; D008024:Ligands; D017448:Receptors, Dopamine D2; C103723:2-(2-benzofuranyl)-2-imidazoline