| Literature DB >> 22489952 |
Sabrina Castellano1, Sabrina Taliani, Ciro Milite, Isabella Pugliesi, Eleonora Da Pozzo, Elisa Rizzetto, Sara Bendinelli, Barbara Costa, Sandro Cosconati, Giovanni Greco, Ettore Novellino, Gianluca Sbardella, Giorgio Stefancich, Claudia Martini, Federico Da Settimo.
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.Entities:
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Year: 2012 PMID： 22489952 DOI： 10.1021/jm201703k
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446