کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10592912 | 981801 | 2014 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Microwave assisted synthesis of naphthopyrans catalysed by silica supported fluoroboric acid as a new class of non purine xanthine oxidase inhibitors
ترجمه فارسی عنوان
سنتز مایکروویو از نفتوپیران های کاتالیز شده توسط اسید فلوئوروبوری اسید سیلیکا به عنوان یک کلاس جدید از مهارکننده های غیر اکسیداز پورین
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
A series of naphthopyrans was synthesized employing silica supported fluoroboric acid under solvent free conditions in a microwave reactor. The catalytic influence of HBF4-SiO2 was investigated in detail to optimize the reaction conditions. The synthesised compounds were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure-activity relationship analyses have also been presented. Among the synthesised compounds, NP-17, NP-19, NP-20, NP-23, NP-24, NP-25 and NP-26 were the active inhibitors with an IC50 ranging from 4 to 17 μM. Compound NP-19 with a thiophenyl ring at position 1 emerged as the most potent xanthine oxidase inhibitor (IC50 = 4 μM) in comparison to allopurinol (IC50 = 11.10 μM) and febuxostat (IC50 = 0.025 μM). The basis of significant inhibition of xanthine oxidase by NP-19 was rationalized by its molecular docking at MTE binding site of xanthine oxidase.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 2, 15 January 2014, Pages 495-500
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 2, 15 January 2014, Pages 495-500
نویسندگان
Sahil Sharma, Kirti Sharma, Ritu Ojha, Dinesh Kumar, Gagandip Singh, Kunal Nepali, P.M.S. Bedi,