946743-11-9Relevant academic research and scientific papers
PLATELET AGGREGATION INHIBITOR, PREPARATION AND USES THEREOF
-
, (2022/03/07)
This disclosure relates to medicines, and more particularly to a platelet aggregation inhibitor, a pharmaceutical composition containing the same and a preparation and application thereof. The platelet aggregation inhibitor provided herein is a compound of formula (I), or a pharmaceutically-acceptable salt, a tautomer or a pharmaceutically-acceptable solvate thereof. This application also provides an application of the compound of formula (I), or a pharmaceutically-acceptable salt, a tautomer, a pharmaceutically-acceptable solvate or a pharmaceutical composition thereof in the treatment of thrombus.
Synthesis and evaluation of 1-hydroxy/methoxy-4-methyl-2-phenyl-1 H-imidazole-5-carboxylic acid derivatives as non-purine xanthine oxidase inhibitors
Chen, Shaolei,Zhang, Tingjian,Wang, Jian,Wang, Fangyang,Niu, Handong,Wu, Chunfu,Wang, Shaojie
, p. 343 - 353 (2015/09/22)
Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid, whose overproduction leads to the gout-causing hyperuricemia. In this study, a series of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives (4ae4k and 6ae6k) was synthesized and evaluated for their inhibitory potency against xanthine oxidase. The 1-hydroxyl substituted derivatives 4ae4k showed excellent inhibitory potency with IC50 values ranging from 0.003 μM to 1.2 μM, with compounds 4d (IC50= 0.003 μM), 4e (IC50 = 0.003 μM), and 4f (IC50 = 0.006 μM) manifesting the most potent xanthine oxidase inhibitory potency that were comparable with that of Febuxostat (IC50 = 0.01 μM). LineweavereBurk plot analysis revealed that representative compound 4f acted as a mixed-type inhibitor for xanthine oxidase. The basis of significant inhibition of xanthine oxidase by 4f was rationalized by its molecular docking into the active site of xanthine dehydrogenase.
INHIBITORS OF ACETYL-COA CARBOXYLASE
-
Page/Page column 39, (2010/11/17)
The present invention relates to compounds that act as acetyl-CoA carboxylase (ACC) inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
