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American Chemical Society, Journal of Medicinal Chemistry, 9(55), p. 4506-4510, 2012

DOI: 10.1021/jm201703k

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

Journal article published in 2012 by Sabrina Castellano, Sabrina Taliani ORCID, Ciro Milite, Isabella Pugliesi, Eleonora Da Pozzo ORCID, Elisa Rizzetto, Sara Bendinelli, Barbara Costa, Sandro Cosconati ORCID, Giovanni Greco, Ettore Novellino, Gianluca Sbardella, Giorgio Stefancich, Claudia Martini ORCID, Federico Da Settimo ORCID
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This paper is available in a repository.

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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 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.