期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 5, 页码 1315-1321出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.01.050
关键词
Xanthine oxidase; High-throughput screening; Hit-to-lead; Non-purine XO inhibitors; Pyrimidone
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. (C) 2014 Elsevier Ltd. All rights reserved.
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