A new guanylhydrazone derivative as a potential acetylcholinesterase inhibitor for Alzheimer's disease: synthesis, molecular docking, biological evaluation and kinetic studies by nuclear magnetic resonance†
a
Marcelle
de Souza Ferreira,
a
Elaine
da Conceição Petronilho,
a
Josélia
Alencar Lima,
a
Sirlene
Oliveira Francisco de Azeredo,
a
Juliana
de Oliveira Carneiro Brum,
a
Claudia
Jorge do Nascimento
b
and
José Daniel
Figueroa Villar
*a
Abstract
The development of pharmacological agents for the treatment of Alzheimer's Disease (AD) is very relevant since this is the most common type of dementia. The inhibition of acetylcholinesterase (AChE) is important to increase the low levels of acetylcholine (ACh) neurotransmitter observed in sick people, which is associated with the memory loss. In this work, a new guanylhydrazone was designed and synthesized as an AChE inhibitor. This new compound was compared to tacrine and other guanylhydrazones. All of them were studied by molecular docking and tested in vitro as AChE inhibitors by Ellman's test and Fig-NMR method. A high inhibition of AChE by the new compound was observed, showing that this compound has great potential for the treatment of AD.
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