6-hydroxyindole and Neurodegenerative-Diseases

6-hydroxyindole has been researched along with Neurodegenerative-Diseases* in 1 studies

Other Studies

1 other study(ies) available for 6-hydroxyindole and Neurodegenerative-Diseases

Article	Year
Indole derivatives as dual-effective agents for the treatment of neurodegenerative diseases: synthesis, biological evaluation, and molecular modeling studies. Bioorganic & medicinal chemistry, 2013, Aug-01, Volume: 21, Issue:15 Several indole derivatives, that were highly potent ligands of GluN2B-subunit-containing N-methyl-D-aspartate (NMDA) receptor, also demonstrated antioxidant properties in ABTS method. In particular, the 2-(4-benzylpiperidin-1-yl)-1-(5-hydroxy-1H-indol-3-yl)ethanone (1) proved to be a dual-effective neuroprotective agent. With the aim to increase the antioxidant properties we added a catechol moiety onto piperidine moiety. The designed hybrid derivative 3,4-dihydroxy-N-[1-[2-(5-hydroxy-1H-indol-3-yl)-2-oxoethyl]piperidin-4-yl]benzamide (10) was the most effective antioxidant agent (>94.1 ± 0.1% of inhibition at 17 μM) and showed GluN2B/NMDA receptor affinity at low micromolar concentration (IC₅₀ 0.66 μM). By means of computational studies we explored the effect of the presence of this antioxidant fragment during the recognition process to binding pocket. Topics: Animals; Antioxidants; Indoles; Male; Models, Molecular; Molecular Docking Simulation; Neurodegenerative Diseases; Radioligand Assay; Rats; Receptors, N-Methyl-D-Aspartate; Structure-Activity Relationship	2013

Article

Year

Indole derivatives as dual-effective agents for the treatment of neurodegenerative diseases: synthesis, biological evaluation, and molecular modeling studies.

Bioorganic & medicinal chemistry, 2013, Aug-01, Volume: 21, Issue:15

Several indole derivatives, that were highly potent ligands of GluN2B-subunit-containing N-methyl-D-aspartate (NMDA) receptor, also demonstrated antioxidant properties in ABTS method. In particular, the 2-(4-benzylpiperidin-1-yl)-1-(5-hydroxy-1H-indol-3-yl)ethanone (1) proved to be a dual-effective neuroprotective agent. With the aim to increase the antioxidant properties we added a catechol moiety onto piperidine moiety. The designed hybrid derivative 3,4-dihydroxy-N-[1-[2-(5-hydroxy-1H-indol-3-yl)-2-oxoethyl]piperidin-4-yl]benzamide (10) was the most effective antioxidant agent (>94.1 ± 0.1% of inhibition at 17 μM) and showed GluN2B/NMDA receptor affinity at low micromolar concentration (IC₅₀ 0.66 μM). By means of computational studies we explored the effect of the presence of this antioxidant fragment during the recognition process to binding pocket.

Topics: Animals; Antioxidants; Indoles; Male; Models, Molecular; Molecular Docking Simulation; Neurodegenerative Diseases; Radioligand Assay; Rats; Receptors, N-Methyl-D-Aspartate; Structure-Activity Relationship

2013