Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 4, Pages 1579-1581Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.138
Keywords
Schizophrenia; Kynurenic acid; Kynurenine; Kynurenine aminotransferase-I; Phenyl hydrazones; Indole propionic acid
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Funding
- The Rebecca L. Cooper Medical Research Foundation
- Selby Research Award
- Australian Postgraduate Award
- University of Sydney
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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 IC50 of 19.8 mu M. (C) 2012 Elsevier Ltd. All rights reserved.
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