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 Chemjournal_title
European journal of medicinal chemistryauthors
Kragler A,Höfner G,Wanner KTdoi
10.1016/j.ejmech.2008.01.005subject
Has Abstractpub_date
2008-11-01 00:00:00pages
2404-11issue
11eissn
0223-5234issn
1768-3254pii
S0223-5234(08)00007-Xjournal_volume
43pub_type
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