Delving into the Latest Updates on Neurodegenerative diseases(Consejo Superior de Investigaciones Científicas) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5-Methoxy-3-(5-methoxyindolin-2-yl)-1H-indole (3)

Target

5-LOX x MAO-A x MAO-B x NQO2

Action

inhibitors

Mechanism

5-LOX inhibitors(Arachidonate 5-lipoxygenase inhibitors), MAO-A inhibitors(Monoamine oxidase A inhibitors), MAO-B inhibitors(Monoamine oxidase B inhibitors)

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Therapeutic Areas

Nervous System Diseases

Active Indication

Neurodegenerative Diseases

Inactive Indication-

Originator Organization-

Active Organization

Consejo Superior de Investigaciones Científicas

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

5-Methoxy-3-(5-methoxyindolin-2-yl)-1H-indole (3), whose structure was unambiguously elucidated by X-ray analysis, was identified as a multi-target compound with potential application in neurodegenerative diseases. It is a low nanomolar inhibitor of QR2 (IC₅₀ = 7.7 nM), with greater potency than melatonin and comparable efficacy to the most potent QR2 inhibitors described to date. Molecular docking studies revealed the potential binding mode of 3 to QR2, which explains its superior potency compared to melatonin. Furthermore, compound 3 inhibits hMAO-A, hMAO-B and hLOX-5 in the low micromolar range and is an excellent ROS scavenger. In phenotypic assays, compound 3 showed neuroprotective activity in a cellular model of oxidative stress damage, it was non-toxic, and was able to activate neurogenesis from neural stem-cell niches of adult mice. These excellent biological properties, together with its both good in silico and in vitro drug-like profile, highlight compound 3 as a promising drug candidate for neurodegenerative diseases.

100 Deals associated with Neurodegenerative diseases(Consejo Superior de Investigaciones Científicas)

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