Synthesis and Biological Evaluation of 4-Phenylquinazoline-2-carboxamides Designed as a Novel Class of Potent Ligands of the Translocator Protein

Castellano, S; Taliani, Sabrina; Milite, C; Pugliesi, I; DA POZZO, Eleonora; Rizzetto, E; Bendinelli, S; Costa, Barbara; Cosconati, S; Greco, G; Novellino, E; Sbardella, G; Stefancich, G; Martini, Claudia; DA SETTIMO PASSETTI, Federico

doi:10.1021/jm201703k

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.

Autori:	Castellano S TALIANI, SABRINA (Secondo) Milite C Pugliesi I DA POZZO, ELEONORA Rizzetto E Bendinelli S COSTA, BARBARA Cosconati S Greco G Novellino E Sbardella G Stefancich G MARTINI, CLAUDIA DA SETTIMO PASSETTI, FEDERICO (Ultimo) mostra contributor esterni nascondi contributor esterni
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

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