216970-75-1

Upstream product

• 55-22-1 pyridine-4-carboxylic acid 
• 23786-14-3 4-methoxy-phenyl acetic acid methyl ester 
• 90322-87-5 1-isonicotinoyl-1H-imidazole 

Downstream Products

• 216970-82-0 3-(4-methoxyphenyl)-6-(4-pyridyl)-3-hydroxy-1-methyl-1H-pyridin-2-one 
• 216970-84-2 3-trifluoromethanesulfonyl-5-(4-methoxyphenyl)-6-(4-pyridyl)-1-methyl-1H-pyridin-2-one 
• 216970-76-2 3-(dimethylamino)-2-(4-methoxyphenyl)-1-(pyridin-4-yl)propen-1-one 
• 216970-80-8 2-benzyloxy-N-[2-(4-methoxy-phenyl)-1-pyridin-4-yl-vinyl]-N-methyl-acetamide 
• 40061-24-3 2-(4-methoxyphenyl)-1-(4-pyridyl)ethan-1-one 

Relevant academic research and scientific papers

A convenient synthesis of highly substituted 2-pyridones

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

3-Heteroaryl-2-pyridones: Benzodiazepine site ligands with functional selectivity for α2/α3-subtypes of human GABAa receptor-ion channels

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

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

Substituted 1H-Pyridinyl-2-ones are useful as GABAA-Alpha 2/3 ligands.