bropirimine and Hyperuricemia

bropirimine has been researched along with Hyperuricemia* in 1 studies

Other Studies

1 other study(ies) available for bropirimine and Hyperuricemia

Article	Year
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase. Bioorganic & medicinal chemistry letters, 2014, Mar-01, Volume: 24, Issue:5 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. Topics: Animals; Binding Sites; Drug Evaluation, Preclinical; Enzyme Activation; Enzyme Inhibitors; Gout Suppressants; Half-Life; High-Throughput Screening Assays; Hyperuricemia; Magnetic Resonance Spectroscopy; Molecular Docking Simulation; Protein Binding; Protein Structure, Tertiary; Pyrimidinones; Rats; Structure-Activity Relationship; Xanthine Oxidase	2014

Article

Year

HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.

Bioorganic & medicinal chemistry letters, 2014, Mar-01, Volume: 24, Issue:5

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.

Topics: Animals; Binding Sites; Drug Evaluation, Preclinical; Enzyme Activation; Enzyme Inhibitors; Gout Suppressants; Half-Life; High-Throughput Screening Assays; Hyperuricemia; Magnetic Resonance Spectroscopy; Molecular Docking Simulation; Protein Binding; Protein Structure, Tertiary; Pyrimidinones; Rats; Structure-Activity Relationship; Xanthine Oxidase

2014