title: Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
abstract: A series of novel 4-phenylquinazoline-2-carboxamides (1-58) were designed as aza-isosters of PK11195, the well-known 18 kDa translocator protein (TSPO) reference ligand, and synthesized by means of a very simple and efficient procedure. A number of these derivatives bind to the TSPO with K(i) values in the nanomolar/subnanomolar range, show selectivity toward the central benzodiazepine receptor (BzR) and exhibit structure-affinity relationships consistent with a previously published pharmacophore/topological model of ligand-TSPO interaction.
authors.affiliation: Dipartimento di Scienze Farmaceutiche e Biomediche, Università di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Castellano
authors.forename: Sabrina
authors.initials: S
authors.lastname: Taliani
authors.forename: Ciro
authors.initials: C
authors.lastname: Milite
authors.forename: Isabella
authors.initials: I
authors.lastname: Pugliesi
authors.forename: Eleonora
authors.initials: E
authors.lastname: Da Pozzo
authors.forename: Elisa
authors.initials: E
authors.lastname: Rizzetto
authors.forename: Sara
authors.initials: S
authors.lastname: Bendinelli
authors.forename: Barbara
authors.initials: B
authors.lastname: Costa
authors.forename: Sandro
authors.initials: S
authors.lastname: Cosconati
authors.forename: Giovanni
authors.initials: G
authors.lastname: Greco
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Gianluca
authors.initials: G
authors.lastname: Sbardella
authors.forename: Giorgio
authors.initials: G
authors.lastname: Stefancich
authors.forename: Claudia
authors.initials: C
authors.lastname: Martini
authors.forename: Federico
authors.initials: F
authors.lastname: Da Settimo
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D002352:Carrier Proteins / Q000378:metabolism*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D002352:Carrier Proteins; D011799:Quinazolines; D011963:Receptors, GABA-A; C069997:Tspo protein, rat