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Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis.

Abstract：

:This article describes discovery of a novel and new class of cholinesterase inhibitors as potential therapeutics for Alzheimer's disease. A series of novel isoalloxazine derivatives were synthesized and biologically evaluated for their potential inhibitory outcome for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds exhibited high activity against both the enzymes AChE as well as BuChE. Of the synthesized compounds, the most potent isoalloxazine derivatives (7m and 7q) showed IC50 values of 4.72 μM and 5.22 μM respectively against AChE; and, 6.98 μM and 5.29 μM respectively against BuChE. These two compounds were further evaluated for their anti-aggregatory activity for β-amyloid (Aβ) in presence and absence of AChE by performing Thioflavin-T (ThT) assay and Congo red (CR) binding assay. In order to evaluate cytotoxic profile of these two potential compounds, cell viability assay of SH-SY5Y human neuroblastoma cells was performed. Further, to understand the binding behavior of these two compounds with AChE and BuChE enzymes, docking studies have been reported.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Kanhed AM,Sinha A,Machhi J,Tripathi A,Parikh ZS,Pillai PP,Giridhar R,Yadav MR

doi

10.1016/j.bioorg.2015.05.005

subject

Has Abstract

pub_date

2015-08-01 00:00:00

pages

7-12

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(15)00043-7

journal_volume

61

pub_type

杂志文章

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