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

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Abstract

A series of 2,4-diaryl-2,3,4,5-tetrahydro- (3640) and 2,4-diaryl-2,3-dihydro-1,5-benzothiazepines (2535) have been synthesized from the corresponding chalcones 124. Both the benzothiazepines and chalcones were evaluated as DPPH free-radical scavengers and as inhibitors of cholinesterases, urease, and α-glucosidase. Compounds 2, 5, 6, 7, 10, 13, 18, 21, 36a, 37a, 37b, and 39a showed significant cholinesterase inhibiting activities. Among the 15 dihydro-1,5-benzothiazepines, 26, 32, and 35 exhibited significant radical-scavenging activities; and six tetrahydro-1,5-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 2731 were found to be potent inhibitors of α-glucosidase.

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