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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Akladios FN,Nadvi NA,Park J,Hanrahan JR,Kapoor V,Gorrell MD,Church WB

doi

10.1016/j.bmcl.2011.12.138

subject

Has Abstract

pub_date

2012-02-15 00:00:00

pages

1579-81

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00027-3

journal_volume

22

pub_type

杂志文章

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