65602-83-7Relevant 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.
