Multitarget compounds bearing tacrine-and donepezil-like structural and functional motifs for the potential treatment of Alzheimer's disease

L Ismaili, B Refouvelet, M Benchekroun, S Brogi… - Progress in …, 2017 - Elsevier
Alzheimer's disease is a multifactorial and fatal neurodegenerative disorder characterized
by decline of cholinergic function, deregulation of other neurotransmitter systems, β-amyloid …

Sigma-2 receptor ligands: neurobiological effects

L Guo, X Zhen - Current medicinal chemistry, 2015 - ingentaconnect.com
Sigma-2 receptor is a widely distributed protein, which can modulate cell proliferation and
involved in the pathogenesis of tumor. Photoaffinity labelling techniques testified that its …

Screening of σ2 Receptor Ligands and In Vivo Evaluation of 11C-Labeled 6,7-Dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline for Potential Use as …

HY Kim, JY Lee, CJ Hsieh, A Riad, NJ Izzo… - Journal of Medicinal …, 2022 - ACS Publications
In this study, a panel of 46 compounds containing five different scaffolds known to have high
σ2 receptor affinity were screened. 6, 7-Dimethoxy-2-[4-(4-methoxyphenyl) butan-2-yl]-1, 2 …

Homology Model and Docking-Based Virtual Screening for Ligands of the σ1 Receptor

E Laurini, VD Col, MG Mamolo… - ACS medicinal …, 2011 - ACS Publications
This study presents for the first time the 3D model of the σ1 receptor protein as obtained from
homology modeling techniques, shows the applicability of this structure to docking-based …

Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for σ1 receptor ligands based on a series of substituted benzo [d] oxazol-2 (3 …

D Zampieri, MG Mamolo, E Laurini… - Journal of medicinal …, 2009 - ACS Publications
Novel benzo [d] oxazol-2 (3 H)-one derivatives were designed and synthesized, and their
affinities against σ receptors were evaluated. On the basis of 31 compounds, a three …

[HTML][HTML] Sigma-1 Receptor Agonists Acting on Aquaporin-Mediated H2O2 Permeability: New Tools for Counteracting Oxidative Stress

G Pellavio, G Rossino, G Gastaldi, D Rossi… - International Journal of …, 2021 - mdpi.com
Sigma1 Receptor (S1R) is involved in oxidative stress, since its activation is triggered by
oxidative or endoplasmic reticulum stress. Since specific aquaporins (AQP), called …

The role of chirality in a set of key intermediates of pharmaceutical interest, 3-aryl-substituted-γ-butyrolactones, evidenced by chiral HPLC separation and by …

D Rossi, R Nasti, S Collina, G Mazzeo… - … of Pharmaceutical and …, 2017 - Elsevier
The enantiomers of four chiral 3-aryl-substituted-γ-butyrolactones, key intermediates for the
preparation of compounds of pharmaceutical interest, were successfully isolated by …

[HTML][HTML] Docking, interaction fingerprint, and three-dimensional quantitative structure–activity relationship (3D-QSAR) of Sigma1 receptor ligands, analogs of the …

JL Velázquez-Libera, G Rossino… - Frontiers in …, 2019 - frontiersin.org
The human Sigma1 receptor (S1R), which has been identified as a target with an important
role in neuropsychological disorders, was first crystallized 3 years ago. Since S1R structure …

Another Brick in the Wall. Validation of the σ1 Receptor 3D Model by Computer-Assisted Design, Synthesis, and Activity of New σ1 Ligands

E Laurini, D Marson, V Dal Col… - Molecular …, 2012 - ACS Publications
Originally considered an enigmatic polypeptide, the σ1 receptor has recently been identified
as a unique ligand-regulated protein. Many studies have shown the potential of σ1 receptor …

A 3D-pharmacophore model for σ2 receptors based on a series of substituted benzo [d] oxazol-2 (3H)-one derivatives

E Laurini, D Zampieri, MG Mamolo, L Vio… - Bioorganic & medicinal …, 2010 - Elsevier
In this work we developed a 3D-pharmacophore model for σ2 receptor based on 19
benzooxazolone derivatives. The best 3D-pharmacophore hypothesis, consisting of five …