288252-01-7Relevant academic research and scientific papers
Synthesis and evaluation of 1-phenyl-1H-1,2,3-triazole-4-carboxylic acid derivatives as xanthine oxidase inhibitors
Zhang, Ting-jian,Wu, Qing-xia,Li, Song-ye,Wang, Lin,Sun, Qi,Zhang, Yi,Meng, Fan-hao,Gao, Hua
, p. 3812 - 3816 (2017)
This study mainly focused on the modification of the X2 position in febuxostat analogs. A series of 1-phenyl-1H-1,2,3-triazole-4-carboxylic acid derivatives (1a-s) with an N atom occupying the X2 position was designed and synthesized. Evaluation of their inhibitory potency in vitro on xanthine oxidase indicated that these compounds exhibited micromolar level potencies, with IC50 values ranging from 0.21?μM to 26.13?μM. Among them, compound 1s (IC50?=?0.21?μM) showed the most promising inhibitory effects and was 36-fold more potent than allopurinol, but was still 13-fold less potent than the lead compound Y-700, which meant that a polar atom fused at the X2 position could be unfavorable for potency. The Lineweaver-Burk plot revealed that compound 1s acted as a mixed-type xanthine oxidase inhibitor. Analysis of the structure-activity relationships demonstrated that a more lipophilic ether tail (e.g., meta-methoxybenzoxy) at the 4′-position could benefit the inhibitory potency. Molecular modeling provided a reasonable explanation for the structure–activity relationships observed in this study.
N-(3-cyano-4-alkoxyphenyl) pyridine carboxamide compound and application thereof
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Paragraph 0075-0076, (2017/08/09)
The invention belongs to the field of medicines, and particularly relates to an N-(3-cyano-4-alkoxyphenyl) pyridine carboxamide compound and application thereof. The N-(3-cyano-4-alkoxyphenyl) pyridine carboxamide compound disclosed by the invention refle
AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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, (2010/01/31)
The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
