Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1579-81. doi: 10.1016/j.bmcl.2011.12.138. Epub 2012 Jan 10.

Design and synthesis of novel inhibitors of human kynurenine aminotransferase-I.

Author information

1
Faculty of Pharmacy A15, The University of Sydney, Sydney, NSW 2006, Australia.

Abstract

Herein we report 6-ethoxy-6-oxo-5-(2-phenylhydrazono) hexanoic acid and 3-(2-carboxyethyl)-1H-indole-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 IC(50) of 19.8 μM.

PMID:
22281190
DOI:
10.1016/j.bmcl.2011.12.138
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center