2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1–mGAT4: Synthesis and biological evaluation

…, GC Höfner, N Guzior, B Filipek, KT Wanner…

文献索引：Kowalczyk, Paula; Salat, Kinga; Hoefner, Georg C.; Guzior, Natalia; Filipek, Barbara; Wanner, Klaus T.; Kulig, Katarzyna Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 17 p. 5154 - 5167

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被引用次数: 8

摘要

Abstract 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 pIC 50 values determined were in the range 4.21–5.14. Two compounds (16a and 16d), ...