8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists

Bioorganic & Medicinal Chemistry Letters
1999.0

Abstract

A series of 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan+ ++-4-one derivatives 1 was studied with respect to the binding affinity for the orphanin FQ (OFQ) and opioid (mu, kappa, delta) receptors. The influence of stereochemistry as well as the substitution pattern of the phenyl-ring in position 1 on the affinity for the orphanin FQ receptor and selectivity to opioid (mu, kappa, delta) receptors is discussed. The most interesting compound 1c was tested for its anxiolytic-like properties in vivo.

Knowledge Graph

Similar Paper

8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists
Bioorganic & Medicinal Chemistry Letters 1999.0
ORL1 receptor ligands: Structure–activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones
Bioorganic & Medicinal Chemistry Letters 2000.0
Structure–activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4′-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide
Bioorganic & Medicinal Chemistry 2009.0
Synthesis and Pharmacology of a Novel κ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton
ACS Medicinal Chemistry Letters 2014.0
Synthesis and Opioid Activity of EnantiomericN-Substituted 2,3,4,4a,5,6,7,7a-Octahydro-1H-benzofuro[3,2-e]isoquinolines
Journal of Medicinal Chemistry 2010.0
Probes for Narcotic Receptor-Mediated Phenomena. 21. Novel Derivatives of 3-(1,2,3,4,5,11-Hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol-6-yl)- phenols with Improved δ Opioid Receptor Selectivity
Journal of Medicinal Chemistry 1996.0
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety
Bioorganic & Medicinal Chemistry Letters 2015.0
Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: Oxygenated N-(2-[1,1′-biphenyl]-4-ylethyl) analogues of 8-CAC
Bioorganic & Medicinal Chemistry Letters 2012.0
C-Alkylated spiro[benzofuran-3(2H),4′-1′-methyl-piperidine-7-ols] as potent opioids: A conformation-activity study
Bioorganic & Medicinal Chemistry Letters 1998.0
Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors
Bioorganic & Medicinal Chemistry Letters 2013.0