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 …

Cognitive decline and BPSD are concomitant with autophagic and synaptic deficits associated with G9a alterations in aged SAMP8 mice

F Vasilopoulou, A Bellver-Sanchis… - Cells, 2022 - mdpi.com
Behavioural and psychological symptoms of dementia (BPSD) are presented in 95% of
Alzheimer's Disease (AD) patients and are also associated with neurotrophin deficits. The …

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] Effect of nacre extract from pearl oyster shells against behavioral and psychological symptoms of dementia in senescence-accelerated mouse P8 (SAMP8)

T Omachi, Y Hasegawa - Journal of Functional Foods, 2024 - Elsevier
Pearls have been used in traditional Chinese medicine for the treatment of myopia, epilepsy,
and palpitations. We previously demonstrated that the intraperitoneal administration of nacre …

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 …

[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 …

Preclinical Evaluation of an Imidazole-Linked Heterocycle for Alzheimer's Disease

A Bagán, S Rodriguez-Arévalo, T Taboada-Jara… - Pharmaceutics, 2023 - mdpi.com
Humanity is facing a vast prevalence of neurodegenerative diseases, with Alzheimer's
disease (AD) being the most dominant, without efficacious drugs, and with only a few …

An Imidazoline 2 Receptor Ligand Relaxes Mouse Aorta via Off-Target Mechanisms Resistant to Aging

F Jiménez-Altayó, A Cabrera, A Bagán… - Frontiers in …, 2022 - frontiersin.org
Imidazoline receptors (IR) are classified into three receptor subtypes (I1R, I2R, and I3R) and
previous studies showed that regulation of I2R signaling has neuroprotective potential. In …

[HTML][HTML] Exploring the reactivity of bicyclic α-iminophosphonates to access new imidazoline I2 receptor ligands

A Bagán, S Abás, J Palà-Pujadas, A Irisarri… - Bioorganic …, 2024 - Elsevier
Recent studies pointed out the modulation of imidazoline I 2 receptors (I 2-IR) by selective
ligands as a putative strategy to face neurodegenerative diseases. Foregoing the classical 2 …

Insights into the Pharmacokinetics and In Vitro Cell-Based Studies of the Imidazoline I2 Receptor Ligand B06

A Bagán, JA Morales-García, C Griñán-Ferré… - International journal of …, 2022 - mdpi.com
The impact of neurodegenerative diseases (ND) is becoming unbearable for humankind
due to their vast prevalence and the lack of efficacious treatments. In this scenario, we …