Compounds > 2-[3-(4-pyridyl)-1H-1-2-4-triazol-5-yl]pyridine

2-[3-(4-pyridyl)-1H-1-2-4-triazol-5-yl]pyridine and Hyperuricemia

2-[3-(4-pyridyl)-1H-1-2-4-triazol-5-yl]pyridine has been researched along with Hyperuricemia* in 1 studies

Other Studies

1 other study(ies) available for 2-[3-(4-pyridyl)-1H-1-2-4-triazol-5-yl]pyridine and Hyperuricemia

Article	Year
Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected]. Bioorganic & medicinal chemistry letters, 2009, Nov-01, Volume: 19, Issue:21 Our previous study identified 2-[2-(2-methoxyethoxy)ethoxy]-5-[5-(2-methyl-4-pyridyl)-1H-[1,2,4] triazol-3-yl]benzonitrile (2)[corrected]as a safe and potent xanthine oxidoreductase (XOR) inhibitor for the treatment of hyperuricemia. Here, we synthesized a series of 3,5-dipyridyl-1,2,4-triazole derivatives and, in particular, examined their in vivo activity in lowering the serum uric acid levels in rats. As a result, we identified 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole (FYX-051, compound 39) [corrected] to be one of the most potent XOR inhibitors; it exhibited an extremely potent in vivo activity, weak CYP3A4-inhibitory activity and a better pharmacokinetic profile than compound 2. Compound 39 is currently being evaluated in a phase 2 clinical trial. Topics: Administration, Oral; Animals; Binding Sites; Crystallography, X-Ray; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Design; Enzyme Inhibitors; Humans; Hyperuricemia; Nitriles; Pyridines; Rats; Structure-Activity Relationship; Xanthine Dehydrogenase	2009

Article

Year

Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected].

Bioorganic & medicinal chemistry letters, 2009, Nov-01, Volume: 19, Issue:21

Our previous study identified 2-[2-(2-methoxyethoxy)ethoxy]-5-[5-(2-methyl-4-pyridyl)-1H-[1,2,4] triazol-3-yl]benzonitrile (2)[corrected]as a safe and potent xanthine oxidoreductase (XOR) inhibitor for the treatment of hyperuricemia. Here, we synthesized a series of 3,5-dipyridyl-1,2,4-triazole derivatives and, in particular, examined their in vivo activity in lowering the serum uric acid levels in rats. As a result, we identified 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole (FYX-051, compound 39) [corrected] to be one of the most potent XOR inhibitors; it exhibited an extremely potent in vivo activity, weak CYP3A4-inhibitory activity and a better pharmacokinetic profile than compound 2. Compound 39 is currently being evaluated in a phase 2 clinical trial.

Topics: Administration, Oral; Animals; Binding Sites; Crystallography, X-Ray; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Design; Enzyme Inhibitors; Humans; Hyperuricemia; Nitriles; Pyridines; Rats; Structure-Activity Relationship; Xanthine Dehydrogenase

2009