The author of 《Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer’s disease》 were Srivastava, Pavan; Tripathi, Prabhash Nath; Sharma, Piyoosh; Shrivastava, Sushant Kumar. And the article was published in Bioorganic & Medicinal Chemistry in 2019. Electric Literature of C6H5Br2N The author mentioned the following in the article:
Novel hybrids N-(4-phenoxybenzyl)aniline were designed, synthesized, and evaluated for their potential AChE inhibitory activity along with antioxidant potential. The inhibitory potential (IC50) of synthesized analogs was evaluated against human cholinesterases (hAChE and hBChE) using Ellman’s method. Among all the tested compounds, 42 with trimethoxybenzene substituent showed maximum hAChE inhibition with the competitive type of enzyme inhibition (IC50 = 1.32 μM; Ki = 0.879 μM). Further, parallel artificial membrane permeation assay (PAMPA-BBB) showed favorable BBB permeability by most of the synthesized compounds Meanwhile, compound 42 also inhibited AChE-induced Aβ aggregation (39.5-66.9%) in thioflavin T assay. The in vivo behavioral studies showed dose-dependent improvement in learning and memory by compound 42. The ex vivo studies also affirmed the significant AChE inhibition and antioxidant potential of compound 42 in brain homogenates. In the experiment, the researchers used 3,5-Dibromoaniline(cas: 626-40-4Electric Literature of C6H5Br2N)
3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Electric Literature of C6H5Br2N
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary