Abed, Dhulfiqar Ali; Lee, Sumi; Wen, Xia; Ali, Ahmed R.; Mangipudy, Vaibhav; Aleksunes, Lauren M.; Hu, Longqin published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Optimization of 1,4-bis(arylsulfonamido)naphthalene-N,N’-diacetic acids as inhibitors of Keap1-Nrf2 protein-protein interaction to suppress neuroinflammation》.Application In Synthesis of Benzyl 2-bromoacetate The article contains the following contents:
The protein-protein interaction (PPI) between kelch-like ECH-associated protein 1 (Keap1) and nuclear factor erythroid 2-related factor 2 (Nrf2) is recognized as a promising target for the prevention and treatment of oxidative stress-related inflammatory diseases. Herein, a series of novel 1,4-bis(arylsulfonamido)naphthalene-N,N’-diacetic acid analogs such as I were designed to further explore the structure-activity relationships of the series. Their activities were measured first with a fluorescence polarization (FP) assay and more potent compounds were further evaluated using a more sensitive time-resolved fluorescence energy transfer (TR-FRET) assay, demonstrating IC50 values between 7.2 and 31.3 nM. In cytotoxicity studies, the naphthalene derivatives did not show noticeable toxicity to human HepG2-C8 and mouse brain BV-2 microglia cells. Among them, I bearing oxygen-containing fused rings was shown to significantly stimulate the cellular Nrf2 signaling pathway, including activation of antioxidant response element (ARE)-controlled expression of Nrf2 target genes and proteins. More importantly, I suppressed up-regulation of several pro-inflammatory cytokines in lipopolysaccharide (LPS)-challenged BV-2 microglial cells, representing a potential therapeutic application for controlling neuroinflammatory disorders.Benzyl 2-bromoacetate(cas: 5437-45-6Application In Synthesis of Benzyl 2-bromoacetate) was used in this study.
Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is a synthetic chemical produced for industry from benzyl alcohol and acetic acid, but is also naturally present in the essential oils of many plants, including jasmine and ylang ylang.Application In Synthesis of Benzyl 2-bromoacetate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary