Discovery and Characterization of a Novel Dihydroisoxazole Class of α-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) Receptor Potentiators was written by Patel, Nandini C.;Schwarz, Jacob;Hou, Xinjun J.;Hoover, Dennis J.;Xie, Longfei;Fliri, Anton J.;Gallaschun, Randall J.;Lazzaro, John T.;Bryce, Dianne K.;Hoffmann, William E.;Hanks, Ashley N.;McGinnis, Dina;Marr, Eric S.;Gazard, Justin L.;Hajos, Mihaly;Scialis, Renato J.;Hurst, Raymond S.;Shaffer, Christopher L.;Pandit, Jayvardhan;O’Donnell, Christopher J.. And the article was included in Journal of Medicinal Chemistry in 2013.Formula: C14H15N3O This article mentions the following:
Pos. allosteric modulators (“potentiators”) of α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors (AMPAR) enhance excitatory neurotransmission and may improve the cognitive deficits associated with various neurol. disorders. The dihydroisoxazole (DHI) series of AMPAR potentiators described herein originated from the identification of one compound by a high-throughput functional activity screen using mouse embryonic stem (mES) cell-derived neuronal precursors. Subsequent structure-based drug design using X-ray crystal structures of the ligand-binding domain of human GluA2 led to the discovery of both PF-04725379, which in tritiated form became a novel ligand for characterizing the binding affinities of subsequent AMPAR potentiators in rat brain homogenate, and PF-04701475 , a prototype used to explore AMPAR-mediated pharmacol. in vivo. Lead series optimization provided a functionally potent compound lacking the potentially bioactivatable aniline within another compound, but retaining desirable in vitro ADME properties. In the experiment, the researchers used many compounds, for example, Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3Formula: C14H15N3O).
Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3) belongs to quinoxaline derivatives. Quinoxaline is isomeric with other naphthyridines including quinazoline, phthalazine and cinnoline. They are well-known for application in organic light emitting devices, polymers and pharmaceutical agents. The quinoxaline-containing polymers are applicable in optical devices due to their thermal stability and low band gap.Formula: C14H15N3O
Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider