Heterocycle-based multicomponent reactions in drug discovery: from hit finding to rational design

P Nadal Rodríguez, O Ghashghaei, A Bagán… - Biomedicines, 2022 - mdpi.com
In the context of the structural complexity necessary for a molecule to selectively display a
therapeutical action and the requirements for suitable pharmacokinetics, a robust synthetic …

Astaxanthin attenuates cognitive deficits in Alzheimer's disease models by reducing oxidative stress via the SIRT1/PGC-1α signaling pathway

N Liu, X Lyu, X Zhang, F Zhang, Y Chen, G Li - Cell & Bioscience, 2023 - Springer
Objective Oxidative stress plays a pivotal role in neurodegenerative diseases. Astaxanthin
(AST) can play a neuroprotective role owing to its long-chain conjugated unsaturated double …

Kai-xin-san inhibits tau pathology and neuronal apoptosis in aged SAMP8 mice

YN Jiao, JS Zhang, WJ Qiao, SY Tian, YB Wang… - Molecular …, 2022 - Springer
Alzheimer's disease (AD) is an age-related neurological disorder. Currently, there is no
effective cure for AD due to its complexity in pathogenesis. In light of the complex …

Disease‐modifying treatment with I2 imidazoline receptor ligand LSL60101 in an Alzheimer's disease mouse model: a comparative study with donepezil

F Vasilopoulou, S Rodríguez‐Arévalo… - British Journal of …, 2021 - Wiley Online Library
Background and Purpose The development of effective therapeutic strategies against
Alzheimer's disease (AD) remains a challenge. I2 imidazoline receptor ligands have a …

[HTML][HTML] Benzofuranyl-2-imidazoles as imidazoline I2 receptor ligands for Alzheimer's disease

S Rodriguez-Arevalo, A Bagan, C Grinan-Ferre… - European journal of …, 2021 - Elsevier
Recent findings unveil the pharmacological modulation of imidazoline I 2 receptors (I 2-IR)
as a novel strategy to face unmet medical neurodegenerative diseases. In this work, we …

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease

S Abás, S Rodriguez-Arevalo, A Bagán… - Journal of medicinal …, 2020 - ACS Publications
Imidazoline I2 receptors (I2-IR), widely distributed in the CNS and altered in patients that
suffer from neurodegenerative disorders, are orphans from a structural point of view, and …

I2-imidazoline ligand CR4056 improves memory, increases ApoE expression and reduces BBB leakage in 5xFAD mice

BC Mota, N Ashburner, L Abelleira-Hervas… - International Journal of …, 2022 - mdpi.com
Recent evidence suggests that I2-imidazoline ligands have neuroprotective properties in
animal models of neurodegeneration, such as Alzheimer's disease (AD). We recently …

I2 imidazoline receptor modulation protects aged SAMP8 mice against cognitive decline by suppressing the calcineurin pathway

F Vasilopoulou, C Grinan-Ferre, S Rodríguez-Arévalo… - GeroScience, 2021 - Springer
Brain aging and dementia are current problems that must be solved. The levels of
imidazoline 2 receptors (I 2-IRs) are increased in the brain in Alzheimer's disease (AD) and …

Agmatine reverses memory deficits induced by Aβ1–42 peptide in mice: A key role of imidazoline receptors

N Kotagale, M Dixit, H Garmelwar, S Bhondekar… - Pharmacology …, 2020 - Elsevier
Abstracts Agmatine is a biogenic amine synthesized following decarboxylation of L-arginine
by the enzyme arginine decarboxylase and exhibits favourable outcome in …

[HTML][HTML] Sex differences in the antidepressant-like response and molecular events induced by the imidazoline-2 receptor agonist CR4056 in rats

E Hernández-Hernández, S Ledesma-Corvi… - Pharmacology …, 2023 - Elsevier
In searching for novel targets to design antidepressants, among the characterized
imidazoline receptors (IR), I2 receptors are an innovative therapeutical approach since they …