40061-24-3Relevant academic research and scientific papers
3-Heteroaryl-2-pyridones: Benzodiazepine site ligands with functional selectivity for α2/α3-subtypes of human GABAa receptor-ion channels
Collins, Ian,Wafford, Keith,Dawson, Gerard R.,Moyes, Christopher,Davey, William B.,Rowley, Michael,Bromidge, Frances A.,Quirk, Kathleen,Atack, John R.,McKernan, Ruth M.,Thompson, Sally-Ann,Pike, Andrew,Sohal, Bindi,Tsou, Nancy N.,Ball, Richard G.,Castro, José L.
, p. 1887 - 1900 (2007/10/03)
A novel series of 3-heteroaryl-5,6-bis(aryl)-1-methyl-2-pyridones were developed with high affinity for the benzodiazepine (BZ) binding site of human γ-aminobutyric acid (GABAA) receptor ion channels, low binding selectivity for α2- and/or α3- over α1-containing GABAA receptor subtypes and high binding selectivity over α5 subtypes. High affinity appeared to be associated with a coplanar conformation of the pyridone and sulfur-containing 3-heteroaryl rings resulting from an attractive S...O intramolecular interaction. Functional selectivity (i.e., selective efficacy) for α2 and/or α3 GABAA receptor subtypes over α1 was observed in several of these compounds in electrophysiological assays. Furthermore, an α3 subtype selective inverse agonist was proconvulsant and anxiogenic in rodents while an α2/α3 subtype selective partial agonist was anticonvulsant and anxiolytic, supporting the hypothesis that subtype selective BZ site agonists may provide new anxiolytic therapies.
SUBSTITUTED 1H-PYRIDINYL-2-ONES AS GABAA ALPHA 2/3 LIGANDS
-
Page column 16, (2010/02/05)
Compounds according to Formula (I) or a salt thereof are selective ligands for GABA A receptors useful for treatment of disorders of the central nervous system:
Substituted 1H-pyridinyl-2-ones as GABAA-α 2/3 ligands
-
, (2008/06/13)
Substituted 1H-Pyridinyl-2-ones are useful as GABAA-Alpha 2/3 ligands.
A convenient synthesis of highly substituted 2-pyridones
Collins, Ian,Castro, Jose L.
, p. 4069 - 4072 (2007/10/03)
A rapid and convenient synthesis of the 3-trifluoromethanesulfonyloxy- 2-pyridone 2, one of the first examples of this class of compound, was achieved by Vilsmeier formylation and cyclisation of the acyl enamine 6. The triflate 2 was found to undergo a ra
An improved and practical procedure for the synthesis of substituted phenylacetylpyridines
Journet, Michel,Cai, Dongwei,Larsen, Robert D.,Reider, Paul J.
, p. 1717 - 1720 (2007/10/03)
A general procedure for the synthesis of substituted phenylacetylpyridines in excellent yields is described using a Horner-Emmons condensation between α-aminoalkylphosphonates of pyridinecarboxaldehydes and benzaldehydes with cesium carbonate at room temperature.
Imidazole derivatives in the treatment of pain
-
, (2008/06/13)
Compounds of the formula SPC1 Wherein R1 represents lower alkyl, cycloalkyl or phenyl which is optionally substituted by halogen, lower alkyl or lower alkoxy, and one of the groups R2 and R3 represents phenyl which is optionally substituted by halogen, lower alkyl, hydroxy, lower alkoxy, lower alkylthio or lower alkylsulphonyl, and the other represents a 6-membered heteroaromatic radical containing 1 or 2 ring nitrogen atoms, their N-oxides and salts, with anti-inflammatory, antinociceptive and antipyretic activity, they are active ingredients of pharmaceutical compositions and can be used for the relief and removal of pain as well as for the treatment of rheumatic, arthritic and other inflammatory complaints; an illustrative example is 2-isopropyl-4(5)-(p-methoxyphenyl)-5(4)-3-pyridyl-imidazole.
