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 Ki 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.

Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein

GRECO, GIOVANNI;NOVELLINO, ETTORE;
2012

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 Ki 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.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11588/626412
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