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Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.

Abstract：

:Six series of 2-substituted 4-aminobutanamide derivatives were synthesized and evaluated for their ability to inhibit GABA transport proteins mGAT1-4 stably expressed in HEK-293 cell lines. The pIC50 values determined were in the range 4.23-5.23. Two compounds (15b and 15c) were selected for further in vitro studies. These compounds were also subjected to preliminary behavioral studies to evaluate their anticonvulsant, antidepressant-like, and antinociceptive activities in mice. Their influence on motor coordination was also assessed. We report that, among a spectrum of in vivo activities, both 15b and 15c displayed significant activity against pentylenetetrazole (PTZ)-induced seizures.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kowalczyk P,Sałat K,Höfner GC,Mucha M,Rapacz A,Podkowa A,Filipek B,Wanner KT,Kulig K

doi

10.1016/j.ejmech.2014.06.024

subject

Has Abstract

pub_date

2014-08-18 00:00:00

pages

256-73

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00543-1

journal_volume

83

pub_type

杂志文章

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