54904-05-1Relevant academic research and scientific papers
Design and synthesis of novel inhibitors of human kynurenine aminotransferase-I
Akladios, Fady N.,Nadvi, Naveed A.,Park, Joohong,Hanrahan, Jane R.,Kapoor, Vimal,Gorrell, Mark D.,Church, W. Bret
supporting information; experimental part, p. 1579 - 1581 (2012/04/04)
Herein we report 6-ethoxy-6-oxo-5-(2-phenylhydrazono) hexanoic acid and 3-(2-carboxyethyl)-1Hindole-2-carboxylic acid derivatives as synthetically accessible leads for human kynurenine aminotransferase-I (KAT-I) inhibitors. In total, 12 compounds were synthesized and their biological activities were determined using the HPLC-UV based KAT-I inhibition assay. Of the 12 compounds synthesized, 10 were found to inhibit human KAT-I and the most active compound was found to be 5-(2-(4-chlorophenyl) hydrazono)-6-ethoxy-6-oxohexanoic acid (9a) with an IC50 of 19.8 lM.
3-(2-Carboxyindol-3-yl)propionic Acid-Based Antagonists of the N-Methyl-D-aspartic Acid Receptor Associated Glycine Binding Site
Salituro, Francesco G.,Harrison, Boyd L.,Baron, Bruce M.,Nyce, Philip L.,Stewart, Kenneth T.,et al.
, p. 1791 - 1799 (2007/10/02)
A series of substituted 3-(2-carboxyindol-3-yl)propionic acids was synthesized and tested as antagonists for the strychnine-insensitive glycine binding site of the NMDA receptor.Chlorine, and other small electron-withdrawing substituents in the 4- and 6-p
BENZOCONDENSED HEPTAATOMIC HETEROCYCLES AND THEIR DERIVATIVES. VII. SYNTHESIS OF BENZAZEPINES AND BENZAZEPINONES ANALOGUES OF KNOWN ANXIOLYTIC DRUGS
Rossi, Silvano,Micheli, Marcello,Giannotti, Michele,Salvatori, Americo,Peruzzi, Guidubaldo
, p. 365 - 370 (2007/10/02)
Two syntheses are described for a series of benzazepines structurally similar to known anxiolytic drugs.Some of the new molecules are active in the barbiturates-induced sleep potentiation test and possess a negligible acute toxicity.
