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 pure antagonists.
Mustazza
Carlo
C
Dipartimento del Farmaco, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy. mustazza@iss.it
Borioni
Anna
A
Sestili
Isabella
I
Sbraccia
Maria
M
Rodomonte
Andrea
A
Ferretti
Rosella
R
Del Giudice
Maria Rosaria
MR
D001593:Benzyl Compounds / Q000737:chemistry; D002460:Cell Line; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D003510:Cyclohexanes / Q000737:chemistry; D015195:Drug Design; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D008745:Methylation; D008958:Models, Molecular; D008968:Molecular Conformation; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists*; D017465:Receptors, Opioid, delta / Q000187:drug effects; D017473:Receptors, Opioid, kappa / Q000187:drug effects; D017450:Receptors, Opioid, mu / Q000187:drug effects; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry; D000094942:Nociceptin Receptor
D001593:Benzyl Compounds; D003510:Cyclohexanes; D008024:Ligands; D011799:Quinazolines; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D013141:Spiro Compounds; D014230:Triazoles; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D000094942:Nociceptin Receptor; C000722283:OPRL1 protein, human