99103-38-5Relevant academic research and scientific papers
Synthesis and bioevaluation of 2-phenyl-5-methyl-2H-1,2,3-triazole-4-carboxylic acid/carbohydrazide derivatives as potent xanthine oxidase inhibitors
Shi, Ailong,Wang, Defa,Wang, He,Wu, Yue,Tian, Haiqiu,Guan, Qi,Bao, Kai,Zhang, Weige
, p. 114879 - 114888 (2016/12/24)
A series of 2-phenyl-5-methyl-2H-1,2,3-triazole-4-carboxylic acids/carbohydrazides as analogues of febuxostat were synthesized and evaluated for their in vitro xanthine oxidase (XO) inhibitory activity. Among these compounds, the carboxylic acid derivatives 7a-h and 8a-h exhibited high potency in the submicromolar/nanomolar range. Steady-state kinetics experiment revealed that 7f was a mixed-type inhibitor of xanthine oxidase. In addition, a molecular docking study of 7f was performed to determine its binding mode at the active site of xanthine oxidase.
Functionalized alkoxy arene diazonium salts from paracetamol
Schmidt, Bernd,Berger, Rene,Hoelter, Frank
supporting information; experimental part, p. 1406 - 1414 (2010/06/19)
Arene diazonium tetrafluoroborates can be synthesized from aromatic acetamides via a sequence of deacetylation, diazotation and precipitation, induced by anion exchange. The reaction is conducted as a convenient one-flask transformation with consecutive addition of the appropriate reagents. Exchange of solvents or removal of byproducts prior to isolation of the product is not required. The arene diazonium salts are isolated from the reaction mixture by simple filtration. Two complementary protocols are presented, and the utility of the reaction is exemplified for a synthesis of the diarylheptanoid natural product de-O-methyl centrolobine.
PHARMACEUTICALLY ACTIVE 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS MODULATORS OF PROTEIN KINASES
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Page/Page column 106, (2010/02/11)
The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof. Furhtermore, the present invention relates to the use of said 4,6-disubstituted aminopyrimidine derivatives as inhibitors for a protein kinase and a medium comprising at least one of said 4,6-disubstituted aminopyrimidine derivatives in an immobilized form and the use of said medium for enriching, purifying and/or depleting nucleotide binding proteins which bind to the immobilized 4,6-disubstituted aminopyrimidine derivatives.
