400752-98-9Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of 1-Benzyl-1H-pyrazole Derivatives as Receptor Interacting Protein 1 Kinase Inhibitors
Zou, Chan,Xiong, Yu,Huang, Lu-Yi,Song, Chun-Li,Wu, Xiao-Ai,Li, Lin-Li,Yang, Sheng-Yong
, p. 569 - 574 (2016)
Receptor interacting protein 1 (RIP1) kinase plays an important role in necroptosis, and inhibitors of the RIP1 kinase are thought to have a potential therapeutic value in the treatment of diseases related to necrosis. Herein, we report the structural optimization of a RIP1 kinase inhibitor, 1-(2,4-dichlorobenzyl)-3-nitro-1H-pyrazole (1a). A number of 1-benzyl-1H-pyrazole derivatives were synthesized and structure-activity relationship (SAR) analysis led to the discovery of a potent compound, 4b, which showed a Kd value of 0.078 μm against the RIP1 kinase and an EC50 value of 0.160 μm in a cell necroptosis inhibitory assay. Compound 4b also displayed considerable ability to protect the pancreas in an l-arginine-induced pancreatitis mouse model.
Benzyl-1H-pyrazole and benzyl-1H-pyrazole derivatives, and preparation method and application thereof
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Paragraph 0057; 0058; 0059; 0060, (2016/10/09)
The invention belongs to the field of chemical medicine, and particularly relates to benzyl-1H-pyrazole and benzyl-1H-pyrazole derivatives, and a preparation method and application thereof. The structure of the benzyl-1H-pyrazole and benzyl-1H-pyrazole de
