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Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.

Abstract：

:A new series of potential GABA uptake inhibitors starting from of 1H-imidazol-4-ylacetic acid with the carboxylic acid side chain originating from different positions and varying in length have been synthesized and tested for the inhibitory potency at the four GABA uptake transporters mGAT1-4 stably expressed in HEK cells. Further two bicyclic compounds with a rigidified carboxylic acid side chain were included in this study. The results of the biological tests indicated that most ω-imidazole alkanoic and alkenoic acid derivatives exhibit the highest potencies as GABA uptake inhibitors at mGAT3.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Hack S,Wörlein B,Höfner G,Pabel J,Wanner KT

doi

10.1016/j.ejmech.2011.01.042

subject

Has Abstract

pub_date

2011-05-01 00:00:00

pages

1483-98

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00064-X

journal_volume

46

pub_type

杂志文章

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