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Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.

Abstract：

:A series of N-substituted aminomethylphenol derivatives was synthesized by reductive amination. To study the inhibitory potency of the target compounds at the murine GABA transporters (mGAT1-mGAT4), a [(3)H]GABA uptake test system in a 96-well format based on HEK cells stably expressing mGAT1-mGAT4 was established and validated. Inhibitory potencies at mGAT1-mGAT4 in the micromolar range and a slight subtype selectivity for mGAT3 were observed for the synthesized aminomethylphenol derivatives. Among the compounds investigated 5-n-dodecylaminomethyl-2-methoxyphenol (21) was found to be most potent with an IC(50) value at mGAT3 of about 3muM.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kragler A,Höfner G,Wanner KT

doi

10.1016/j.ejmech.2008.01.005

subject

Has Abstract

pub_date

2008-11-01 00:00:00

pages

2404-11

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(08)00007-X

journal_volume

43

pub_type

杂志文章

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