کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364239 981532 2007 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors
چکیده انگلیسی

Xanthine oxidase (XO) is a key enzyme which can catalyze xanthine to uric acid causing hyperuricemia in humans. By using the fractionation technique and inhibitory activity assay, an active compound that prevents XO from reacting with xanthine was isolated from wheat leaf. It was identified by the Mass and NMR as 6-aminopurine (adenine). A structure–activity study based on 6-aminopurine was conducted. The inhibition of XO activity by 6-aminopurine (IC50 = 10.89 ± 0.13 μM) and its analogues was compared with that by allopurinol (IC50 = 7.82 ± 0.12 μM). Among these analogues, 2-chloro-6(methylamino)purine (IC50 = 10.19 ± 0.10 μM) and 4-aminopyrazolo[3,4-d] pyrimidine (IC50 = 30.26 ± 0.23 μM) were found to be potent inhibitors of XO. Kinetics study showed that 2-chloro-6(methylamino)purine is non-competitive, while 4-aminopyrazolo[3,4-d]pyrimidine is competitive against XO.

The 6-aminopurine and its analogues were evaluated as xanthine oxidase inhibitors. These inhibitors are likely to be adopted as candidates to treat gout.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 10, 15 May 2007, Pages 3450–3456
نویسندگان
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