کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584703 | 981347 | 2012 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase
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کلمات کلیدی
PMPSSAGADPLPGABA-ATSynthetic substratesγ-aminobutyric acid - اسید γ-آمینوبوتیریکHeteroaromatic compounds - ترکیبات نیتروارویتیBBB - سد خونی مغزیBlood–brain barrier - سد خونی مغزیsuccinic semialdehyde - سمیالدئید بنسنیکینEnzyme inhibition - مهار آنزیمpyridoxal 5′-phosphate - پیریدوکسال 5'-فسفاتGABA - گاباGABA aminotransferase - گابا آمینوترانسفراز
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase](/preview/png/10584703.png)
چکیده انگلیسی
Two principal neurotransmitters are involved in the regulation of mammalian neuronal activity, namely, γ-aminobutyric acid (GABA), an inhibitory neurotransmitter, and l-glutamic acid, an excitatory neurotransmitter. Low GABA levels in the brain have been implicated in epilepsy and several other neurological diseases. Because of GABA's poor ability to cross the blood-brain barrier (BBB), a successful strategy to raise brain GABA concentrations is the use of a compound that does cross the BBB and inhibits or inactivates GABA aminotransferase (GABA-AT), the enzyme responsible for GABA catabolism. Vigabatrin, a mechanism-based inactivator of GABA-AT, is currently a successful therapeutic for epilepsy, but has harmful side effects, leaving a need for improved GABA-AT inactivators. Here, we report the synthesis and evaluation of a series of heteroaromatic GABA analogues as substrates of GABA-AT, which will be used as the basis for the design of novel enzyme inactivators.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 19, 1 October 2012, Pages 5763-5773
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 19, 1 October 2012, Pages 5763-5773
نویسندگان
Dustin D. Hawker, Richard B. Silverman,