کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10586732 981395 2011 13 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: Synthesis and biological evaluation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: Synthesis and biological evaluation
چکیده انگلیسی
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 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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 21, 1 November 2011, Pages 6492-6504
نویسندگان
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