Synthesis and Evaluation as NOP Ligands of Some Spiro[piperidine-4,2′(1′H)-quinazolin]-4′(3′H)-ones and Spiro[piperidine-4,5′(6′H)-[1,2,4]triazolo[1,5-c]quinazolines]

Some spiro[piperidine-4,2′(1′H)-quinazolin]-4′(3′H)-ones 3 and spiro[piperidine-4,5′(6′H)-[1,2,4]triazolo[1,5-c]quinazolines] 4 were synthesized and evaluated as ligands of the nociceptin receptor. The examined compounds showed partial agonistic activity, except compounds 3, 4n that proved to be pur...

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Veröffentlicht in:	Chemical & Pharmaceutical Bulletin 2006, Vol.54(5), pp.611-622
Hauptverfasser:	Mustazza, Carlo, Borioni, Anna, Sestili, Isabella, Sbraccia, Maria, Rodomonte, Andrea, Ferretti, Rosella, Giudice, Maria Rosaria Del
Format:	Artikel
Sprache:	eng
Schlagworte:	Benzyl Compounds - chemistry Cell Line Cell Membrane - drug effects Cell Membrane - metabolism Cyclohexanes - chemistry Drug Design Guanosine 5'-O-(3-Thiotriphosphate) - pharmacology Humans Ligands Methylation Models, Molecular Molecular Conformation nociceptin receptor ligand opioid Quinazolines - chemical synthesis Quinazolines - pharmacology Receptors, Opioid - agonists Receptors, Opioid, delta - drug effects Receptors, Opioid, kappa - drug effects Receptors, Opioid, mu - drug effects Spiro Compounds - chemical synthesis Spiro Compounds - pharmacology spiropiperidine spiropiperidine triazoloquinazoline Structure-Activity Relationship Triazoles - chemistry
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Zusammenfassung:	Some spiro[piperidine-4,2′(1′H)-quinazolin]-4′(3′H)-ones 3 and spiro[piperidine-4,5′(6′H)-[1,2,4]triazolo[1,5-c]quinazolines] 4 were synthesized and evaluated as ligands of the nociceptin receptor. The examined compounds showed partial agonistic activity, except compounds 3, 4n that proved to be pure antagonists.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.54.611