Syntheses and Biological Activities of Chalcone and 1,5-Benzothiazepine Derivatives: Promising New Free-Radical Scavengers,and Esterase,Urease, and alpha-Glucosidase Inhibitors

摘要

A series of 2,4-diaryl-2,3,4,5-tetrahydro- (36-40) and 2,4-diaryl-2,3-dihydro-l,5-benzothiazepines (25-35) have been synthesized from the corresponding chalcones 1-24.Both the benzothiazepines and chalcones were evaluated as DPPH free-radical scavengers and as inhibitors of cholinesterases,urease,and alpha-glucosidase.Compounds 2,5,6,7,10,13,18,21,36a,37a,37b,and 39a showed significant cholinesterase inhibiting activities.Among the 15 dihydro-l,5-benzothiazepines,26,32,and 35 exhibited significant radical-scavenging activities;and six tetrahydro-l,5-benzothiazepines (35,36a,36b,37a,37b,and 39a) were found to be inhibitors of AChE and BChE.Compounds 22,25,26,33,35,36a,37b,and 39a inhibited urease,and 25 and 27-31 were found to be potent inhibitors of a-glucosidase.