19353-97-0Relevant articles and documents
Surveying heterocycles as amide bioisosteres within a series of mGlu7 NAMs: Discovery of VU6019278
Reed, Carson W.,Washecheck, Jordan P.,Quitlag, Marc C.,Jenkins, Matthew T.,Rodriguez, Alice L.,Engers, Darren W.,Blobaum, Anna L.,Jeffrey Conn,Niswender, Colleen M.,Lindsley, Craig W.
, p. 1211 - 1214 (2019/03/26)
This letter describes a diversity-oriented library approach to rapidly assess diverse heterocycles as bioisosteric replacements for a metabolically labile amide moiety within a series of mGlu7 negative allosteric modulators (NAMs). SAR rapidly
Design, synthesis, and pharmacological and pharmacokinetic evaluation of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives as xanthine oxidoreductase inhibitors
Sato, Takahiro,Ashizawa, Naoki,Iwanaga, Takashi,Nakamura, Hiroshi,Matsumoto, Koji,Inoue, Tsutomu,Nagata, Osamu
scheme or table, p. 184 - 187 (2009/05/26)
In an effort to find a potent xanthine oxidoreductase (XO) inhibitor, we discovered the best compound 2-[2-(2-methoxy-ethoxy)-ethoxy]-5-[5-(2-methyl-pyridin-4-yl)-1H-[1,2,4]triazol-3-yl]-benzonitrile 28. Here, we describe the following: (1) the design, synthesis, and structure-activity relationship of a series of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives by in vitro studies of XO inhibitory activity in bovine milk and in vivo studies of serum uric acid (UA) reductive activity in rats, (2) a drug interaction study by a cytochrome P450 3A4 (CYP3A4) assay, and (3) a pharmacokinetic (PK) study. Compound 28 exhibits potent XO inhibitory activity, serum UA-lowering activity in rats, weak CYP3A4 inhibitory activity, and moderate PK profile.
MGLUR5 MODULATORS II
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Page/Page column 20, (2008/06/13)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.