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.
TALIANI, SABRINA (Secondo) (Corresponding)
DA SETTIMO PASSETTI, FEDERICO (Ultimo)
|Autori:||Castellano, S; Taliani, Sabrina; Milite, C; Pugliesi, I; DA POZZO, Eleonora; Rizzetto, E; Bendinelli, S; Costa, Barbara; Cosconati, S; G, Greco; Novellino, E; Sbardella, G; Stefancich, G; Martini, Claudia; DA SETTIMO PASSETTI, Federico|
|Titolo:||Synthesis and Biological Evaluation of 4-Phenylquinazoline-2-carboxamides Designed as a Novel Class of Potent Ligands of the Translocator Protein|
|Anno del prodotto:||2012|
|Digital Object Identifier (DOI):||10.1021/jm201703k|
|Appare nelle tipologie:||1.1 Articolo in rivista|