288252-05-1Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 5-(4-(pyridin-4-yl)-1H-1,2,3-triazol-1-yl)benzonitrile derivatives as xanthine oxidase inhibitors
Zhang, Ting-Jian,Li, Song-Ye,Zhang, Yi,Wu, Qing-Xia,Meng, Fan-Hao
, p. 526 - 533 (2018)
A series of 5-(4-(pyridin-4-yl)-1H-1,2,3-triazol-1-yl)benzonitrile derivatives (1a–p) was designed, synthesized, and identified as xanthine oxidase inhibitors with micromolar level potencies. Among them, the most promising compounds 1j and 1k were obtained with IC50 values of 8.1 and 6.7?μm, respectively. The Lineweaver–Burk plot revealed that compound 1k acted as a mixed-type xanthine oxidase inhibitor. SAR analysis revealed that a carbon atom occupying the X3 position is not as effective as a nitrogen atom, and an iso-pentyloxy or a cyclopentyloxy at the 2-position of benzonitrile moiety will benefit the inhibitory potency. The basis of xanthine oxidase inhibition by 1k was rationalized by molecular modeling studies.
1-substituted phenyl-1H-1,2,3-triazole compound as well as preparation method and application thereof
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Paragraph 0018; 0037, (2016/11/17)
The invention relates to a 1-substituted phenyl-1H-1,2,3-triazole compound, in particular to a compound applicable to preparation of anti-gout drugs and a preparation method of the compound, and belongs to the field of medicines. The compound is as shown in the general formula, wherein each R1 is independent alkyl of 1-10 carbons, 3-10 carbon atom naphthenic bases, allyl, methoxy ethyl, benzyl and substituted benzyl; substituted benzyl can be p-halogenated benzyl, p-cyano benzyl and p-alkoxy benzyl; each R2 is independent H or methyl; each R3 is independent H or ethyl. Experimental results show that the compound has a good effect in the in-vitro xanthine oxidase inhibition activity test.
AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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Page 61, (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.
