285984-22-7Relevant articles and documents
POLYAROMATIC UREA DERIVATIVES AND THEIR USE IN THE TREATMENT OF MUSCLE DISEASES
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Page/Page column 137-138, (2021/01/29)
The current invention provides urea derivatives, in particular compounds having the core structure heteroaryl-NH-CO-NH-aryl-O- heteroaryl, for use in treating, ameliorating, delaying, curing and/ or preventing a disease or condition associated with muscle cells and/or satellite cells, such as Duchenne muscular dystrophy, Becker muscular dystrophy, cachexia or sarcopenia.
Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions
Lu, Meng-Chen,Shao, Hong-Li,Liu, Tian,You, Qi-Dong,Jiang, Zheng-Yu
supporting information, (2020/09/01)
Nuclear factor erythroid 2-related factor 2 (NRF2) is a pleiotropic transcription factor which regulates the constitutive and inducible transcription of a wide array of genes and confers protection against a variety of pathologies. Directly disrupting Kelch-like ECH-associated protein 1 (KEAP1)-NRF2 protein-protein interaction (PPI) has been explored as a promising strategy to activate NRF2. We reported here the first identification of a series of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 inhibitors. Our efforts led to the potent small molecule KEAP1-NRF2 inhibitor, 20c, which exhibited a Kd of 24 nM to KEAP1 and an IC50 of 75 nM in disrupting KEAP1-NRF2 interaction. Subsequent biological studies provided consistent evidence across mouse macrophage cell-based and in vivo models that 20c induced NRF2 target gene expression and enhanced downstream antioxidant and anti-inflammatory activities. Our study not only demonstrated that small molecule KEAP1-NRF2 PPI inhibitors can be potential preventive and therapeutic agents for diseases and conditions involving oxidative stress and inflammation but also enriched the chemical diversity of the KEAP1-NRF2 inhibitors.
1-sulfonamide-4-aryloxy compound, preparation method and medical application of 1-sulfonamide-4-aryloxy compound
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Paragraph 0063; 0064, (2016/12/22)
The invention relates to the field of medicinal chemistry, in particular to a compound (I) with 1-sulfonamide-4-aryloxy being a basis framework. The compound has anti-inflammatory activity. A primary activity test proves that the compound has good interference Keap1-Nrf2 combination, so that Nrf2 is activated, and the compound has potential anti-inflammatory activity and can be used for treating numerous inflammation-related diseases including the chronic obstructive pulmonary disease (COPD), the Alzheimer's disease, Parkinson, atherosclerosis, the chronic renal disease (CKD), diabetes, intestine inflammations, rheumatoid arthritis and the like. (Please see the description for the formula I.).