14378-08-6Relevant articles and documents
Enhanced antioxidation capacity endowed to a mixed type aldose reductase inhibitor leads to a promising anti-diabetic complications agent
Liu, Yuanlin,Mo, Hui,Zhang, Kun,Yin, Meili,Yuan, Sheng,Li, Yanbing,Li, Yifang,Zhu, Wenda,Fan, Yiping,Zeng, Yancong,Kurihara, Hiroshi,He, Rongrong,Chen, Heru
, (2022/01/24)
A series of 5f-based new compounds has been designed and synthesized. In vitro screening demonstrated that the binding affinity and selectivity on aldose reductase (AR) were positively correlated with its antioxidation capacity. Compound 6d was verified t
Synthesis and biological evaluation of bifendate derivatives bearing acrylamide moiety as novel antioxidant agents
Gu, Xiaoke,Jiang, Yanfei,Chen, Jing,Zhang, Yinpeng,Guan, Mingyu,Li, Xin,Zhou, Qingqing,Lu, Qian,Qiu, Jingying,Yin, Xiaoxing
, p. 59 - 69 (2018/11/21)
Oxidative stress plays a significant role in the pathogenesis of various human diseases. In this study, a series of bifendate derivatives bearing acrylamide moiety were synthesized and evaluated as anti-oxidant agents. Biological evaluation indicated that
Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases
Nitsche, Christoph,Steuer, Christian,Klein, Christian D.
experimental part, p. 7318 - 7337 (2012/01/05)
The 3-aryl-2-cyanoacrylamide scaffold was designed as core pharmacophore for inhibitors of the Dengue and West Nile virus serine proteases (NS2B-NS3). A total of 86 analogs was prepared to study the structure-activity relationships in detail. Thereby, it turned out that the electron density of the aryl moiety and the central double bond have a crucial influence on the activity of the compounds, whereas the influence of substituents of the amide residue is less relevant. The para-hydroxy substituted analog was found to be the most potent inhibitor in this series with a Ki-value of 35.7 μM at the Dengue and 44.6 μM at the West Nile virus protease. The aprotinin competition assay demonstrates a direct interaction of the inhibitor molecule with active centre of the Dengue virus protease. The target selectivity was studied in a counterscreen with thrombin and found to be 2.8:1 in favor of DEN protease and 2.3:1 in favor of WNV protease, respectively.