Design and Bioevaluation of Novel Hydrazide-Hydrazones Derived from 4-Acetyl-N-Substituted Benzenesulfonamide

Abstract

In this research, a series of hydrazine-hydrazone derivatives (Ia-g), (IIa-h) were synthesized to discover new antioxidant and anticholinesterase agents. The structures of synthesized compounds were characterized by spectroscopic data using UV, IR, H-1, C-13 NMR, mass spectroscopy, and elemental analysis. The bio-evaluation of the synthesized compounds (Ia-g), (IIa-h) were evaluated according to in vitro activity assays. The results of beta-carotene/linoleic acid assay showed that among the synthesized compounds, the (Ib), (Ie), (IIb-IIe), and (IIh) compound exhibited higher activity for the lipid peroxidation inhibitory activity. In the DPPH free scavenging activity and the cation radical scavenging activity in ABTS(center dot+) activity, compound (IIb) was found to be more active. In the CUPRAC reduced power assay, the A(0.5) values of all synthesized compounds were better than alpha-TOC. In AChE assay, compound (IIb) exhibited the most activity with IC50 = 11.12 +/- 0.74 mu M, while the compounds (Ib-g) and (IIb-h), exhibited excellent activity than the positive standard galantamine (IC50 = 46.06 +/- 0.10 mu M) in the BChE assay.