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Título

A therapeutic approach to cerebrovascular diseases based on indole substituted hydrazides and hydrazines able to interact with human vascular adhesion protein-1, monoamine oxidases (A and B), AChE and BuChE

Autor Esteban, Gerard; Bolea, Irene; Sun, Ping; Solé, Montserrat ; Samadi, Abdelouahid ; Marco-Contelles, José ; Unzeta, Mercedes
Palabras clave Hydrazine
Hydrazide
Monoamine oxidase
Vascular adhesion protein-1
Acetylcholinesterase
Fecha de publicación 2013
EditorSpringer
Citación Journal of Neural Transmission 120: 911- 918 (2013)
ResumenHerein, we report the biological evaluation of a series of indole substituted hydrazides and hydrazines throughout the assessment of their multipotent inhibitory potency towards monoamine oxidase (MAO) A and B, semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1), and the cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Hydrazine JL72 (3-(3-hydrazinylpropyl)-1H-indole) showed a potent, reversible and non-time-dependent inhibition of MAO-A, which suggests its capacity in restoring serotoninergic neurotransmission being devoid of the side effects observed for classic MAO-A inhibitors. In addition, JL72 behaved as a moderate BuChE inhibitor. Finally, both hydrazines and hydrazides derivatives showed high affinity towards SSAO/VAP-1. Among them, JL72 behaved as a noncompetitive and the most potent inhibitor (IC50 = 0.19 ± 0.04 μM), possessing also a significant anti-inflammatory activity. The combined inhibition of SSAO/VAP-1, MAO (A and B), AChE and BuChE appear as an important therapeutic target to be considered in the treatment of cerebrovascular and neurological disorders such as Alzheimer's disease. © 2012 Springer-Verlag Wien.
URI http://hdl.handle.net/10261/94953
DOI10.1007/s00702-012-0949-x
Identificadoresdoi: 10.1007/s00702-012-0949-x
issn: 0300-9564
e-issn: 1435-1463
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