Synthesis, Type II diabetes inhibitory activity, antimicrobial evaluation and docking studies of indeno[1,2-]pyrazol-4(1)-ones.
Journal:
Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents
Published Date:
Oct 26, 2019
Abstract
We report a convenient and efficient synthesis of indeno[1,2-]pyrazol-4(1)-ones () by the reaction of a variety of 2-acyl-(1)-indene-1,3(2)-diones () and 2-hydrazinylbenzo[]thiazole/2-hydrazinyl-6-substitutedbenzo[]thiazoles () in the presence of glacial acetic acid in good yields. The structure of the compounds thus prepared were confirmed by analytical and spectral (FT-IR, H NMR, C NMR, and HRMS) techniques. All the synthesized indeno[1,2-]pyrazol-4(1)-ones () were assayed for their in vitro Type II diabetes inhibitory activity by using Acarbose as standard drug and in vitro antimicrobial activity utilizing Streptomycin and Fluconazole as reference drugs. Among the synthesized derivatives, (IC = 6.71 μg/mL) was found to be more potent against -glucosidase enzyme as compared with the standard Acarbose (IC = 9.35 μg/mL) and (IC = 11.90 μg/mL) exhibited good inhibitory activity against -amylase enzyme as compared with the standard Acarbose (IC = 22.87 μg/mL). Also, all the titled compounds showed good antimicrobial activity. In addition, in vitro α-glucosidase and -amylase inhibition were supported by docking studies performed on the derivatives and , respectively.
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