1449792-86-2Relevant academic research and scientific papers
2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: Synthesis and biological evaluation
Kowalczyk, Paula,Sa?at, Kinga,H?fner, Georg C.,Guzior, Natalia,Filipek, Barbara,Wanner, Klaus T.,Kulig, Katarzyna
, p. 5154 - 5167 (2013/09/02)
A series of 2-substituted 4-hydroxybutanamide derivatives has been synthesized by the aminolysis of appropriate 2-substituted dihydrofuran-2(3H)- one derivatives with various substituted benzylamines. The final compounds have been evaluated for their capability of inhibiting the GABA transport proteins GAT1-4 stably expressed in HEK-239 cell lines. The pIC50 values determined were in the range 4.21-5.14. Two compounds (16a and 16d), which displayed the most interesting profiles in in vitro tests, have also been subjected to further preliminary behavioral studies, evaluating their antinociceptive activity in hot-plate, writhing, and formalin tests. Their influence on motor coordination has also been assessed.
