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
CASTELLANO, Sabrina;MILITE, CIRO;SBARDELLA, Gianluca;
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.File in questo prodotto:
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