Bioorganic & medicinal chemistry

Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1–mGAT4: Synthesis and biological evaluation

ES Schaffert, G Höfner, KT Wanner

文献索引：Schaffert, Eva S.; Hoefner, Georg; Wanner, Klaus T. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6492 - 6504

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被引用次数: 20

摘要

1, 5-Disubstituted and 5-monosubstituted aminomethyltetrazole derivatives derived from glycine were synthesized employing a TMSN3-modified variant of the Ugi reaction as a key step. All compounds were evaluated regarding their inhibitory potency and subtype selectivity at the four murine GABA transporter subtypes mGAT1–mGAT4. Though none of the 5-monosubstituted tetrazoles turned out to inhibit [3H] GABA uptake to a significant ...