28177-79-9Relevant articles and documents
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
supporting information, p. 3812 - 3816 (2017/07/27)
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.
NOVEL AMIDE COMPOUNDS WITH MCH ANTAGONISTIC EFFECT AND MEDICAMENTS COMPRISING SAID COMPOUNDS
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Page/Page column 88, (2008/06/13)
The invention relates to amide compounds of general formula (I), in which the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. The invention further relates to medicaments comprising at least one of said amides. Said medicaments are suitable for the treatment of metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia, and diabetes as a result of the MCH receptor antagonism.
IL-8 RECEPTOR ANTAGONISTS
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, (2008/06/13)
Novel IL-8 receptor antagonists and methods of using them are provided.