nnc-05-2090 and Central-Nervous-System-Diseases

nnc-05-2090 has been researched along with Central-Nervous-System-Diseases* in 1 studies

Other Studies

1 other study(ies) available for nnc-05-2090 and Central-Nervous-System-Diseases

Article	Year
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. Bioorganic & medicinal chemistry, 2011, Nov-01, Volume: 19, Issue:21 1,5-Disubstituted and 5-monosubstituted aminomethyltetrazole derivatives derived from glycine were synthesized employing a TMSN(3)-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 [(3)H]GABA uptake to a significant extent, the 1,5-disubstituted tetrazole derivatives displayed a distinct activity, especially at the GABA transport proteins mGAT2-mGAT4. Thus, a reasonable potent and selective inhibitor of mGAT3 was found. Additionally, two more compounds were identified as potent inhibitors of mGAT2. This is especially relevant, as up to date only few potent inhibitors of mGAT2 that do not affect mGAT1 are known. Topics: Animals; Cell Line; Central Nervous System Diseases; GABA Plasma Membrane Transport Proteins; GABA Uptake Inhibitors; Glycine; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mice; Molecular Structure; Spectroscopy, Fourier Transform Infrared; Structure-Activity Relationship; Tandem Mass Spectrometry; Tetrazoles	2011

Article

Year

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

Bioorganic & medicinal chemistry, 2011, Nov-01, Volume: 19, Issue:21

1,5-Disubstituted and 5-monosubstituted aminomethyltetrazole derivatives derived from glycine were synthesized employing a TMSN(3)-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 [(3)H]GABA uptake to a significant extent, the 1,5-disubstituted tetrazole derivatives displayed a distinct activity, especially at the GABA transport proteins mGAT2-mGAT4. Thus, a reasonable potent and selective inhibitor of mGAT3 was found. Additionally, two more compounds were identified as potent inhibitors of mGAT2. This is especially relevant, as up to date only few potent inhibitors of mGAT2 that do not affect mGAT1 are known.

Topics: Animals; Cell Line; Central Nervous System Diseases; GABA Plasma Membrane Transport Proteins; GABA Uptake Inhibitors; Glycine; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mice; Molecular Structure; Spectroscopy, Fourier Transform Infrared; Structure-Activity Relationship; Tandem Mass Spectrometry; Tetrazoles

2011