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EnglishA 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.
| Titolo: | Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein | |
| Autori: | ||
| Data di pubblicazione: | 2012 | |
| Rivista: | ||
| 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. | |
| Handle: | http://hdl.handle.net/11588/626412 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
File in questo prodotto:
| File | Descrizione | Tipologia | Licenza | |
|---|---|---|---|---|
| j med chem_2012_55_4506.pdf | Articolo principale | Documento in Post-print | Accesso privato/ristretto | Utenti riconosciuti Richiedi una copia |
http://hdl.handle.net/11588/626412
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