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)
DA SETTIMO PASSETTI, FEDERICO (Ultimo)
|Autori:||Castellano S; Taliani S; Milite C; Pugliesi I; Da Pozzo E; Rizzetto E; Bendinelli S; Costa B; Cosconati S; Greco G; Novellino E; Sbardella G; Stefancich G; Martini C; Da Settimo F|
|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|