کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369901 | 981793 | 2014 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The identification of novel, non-purine based inhibitors of xanthine oxidase is described. After a high-throughput screening campaign, an NMR based counterscreen was used to distinguish actives, which interact with XO in a reversible manner, from assay artefacts. This approach identified pyrimidone 1 as a reversible and competitive inhibitor with good lead-like properties. A hit to lead campaign gave compound 41, a nanomolar inhibitor of hXO with efficacy in the hyperuricemic rat model after oral dosing.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 5, 1 March 2014, Pages 1315–1321
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 5, 1 March 2014, Pages 1315–1321
نویسندگان
Johan Evenäs, Fredrik Edfeldt, Matti Lepistö, Naila Svitacheva, Anna Synnergren, Britta Lundquist, Mia Gränse, Anna Rönnholm, Mikael Varga, John Wright, Min Wei, Sherrie Yue, Junfeng Wang, Chong Li, Xuan Li, Gang Chen, Yong Liao, Gang Lv, Ann Tjörnebo,