Synthesis, Structure and Evaluation of the N-(2-Acetyl-4-(styryl)phenyl)-4-benzenesulfonamide Derivatives for Anticholinesterase and Antioxidant Activities

摘要: N-(2-Acetyl-4-bromophenyl)-4-methylbenzenesulfonamide (2) was transformed into 5-(4-methoxymethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3a) and 5-(4- trifluoromethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3b). Their structures were determined using a combination of NMR (1H & 13C) mass spectroscopic as well single crystal X-ray diffraction techniques. These compounds the corresponding precursor, 2-amino-5-bromoacetophenone (1), evaluated through enzymatic assays in vitro for inhibitory effect against acetylcholinesterase (AChE) butyrylcholinesterase (BChE) activities antioxidant 2,2-diphenyl-1-picrylhydrazyl (DPPH) nitric oxide (NO) free radical scavenging assays. Molecular docking performed on 3a to determine plausible protein–ligand interactions molecular level. drug likeness properties (absorption, distribution, metabolism, excretion) ability cross blood–brain barrier (BBB) have also been predicted at theoretical