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Indene-Derived Hydrazides Targeting Acetylcholinesterase Enzyme in Alzheimer's: Design, Synthesis, and Biological Evaluation.

Authors :
Gupta, Shraddha Manish
Behera, Ashok
Jain, Neetesh K.
Kumar, Devendra
Tripathi, Avanish
Tripathi, Shailesh Mani
Mujwar, Somdutt
Patra, Jeevan
Negi, Arvind
Source :
Pharmaceutics. Jan2023, Vol. 15 Issue 1, p94. 11p.
Publication Year :
2023

Abstract

As acetylcholinesterase (AChE) plays a crucial role in advancing Alzheimer's disease (AD), its inhibition is a promising approach for treating AD. Sulindac is an NSAID of the aryl alkanoic acid class, consisting of a indene moiety, which showed neuroprotective behavior in recent studies. In this study, newer Indene analogs were synthesized and evaluated for their in vitro AChE inhibition. Additionally, compared with donepezil as the standard drug, these Indene analogs were accessed for their cell line-based toxicity study on SH-SY5Y cell line. The molecule SD-30, having hydrogen bond donor (HBD) at para-position, showed maximum AChE inhibition potential (IC50 13.86 ± 0.163 µM) in the indene series. Further, the SD-30 showed maximum BuChE inhibition potential (IC50 = 48.55 ± 0.136 µM) with a selectivity ratio of 3.50 and reasonable antioxidant properties compared to ascorbic acid (using DPPH assay). SD-30 (at a dose level: of 10 µM, 20 µM) effectively inhibited AChE-induced Aβ aggregation and showed no significant toxicity up to 30 mM against SH-SY5Y cell lines. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
19994923
Volume :
15
Issue :
1
Database :
Academic Search Index
Journal :
Pharmaceutics
Publication Type :
Academic Journal
Accession number :
161481803
Full Text :
https://doi.org/10.3390/pharmaceutics15010094