[HTML][HTML] 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 …

[HTML][HTML] Targeting CaN/NFAT in Alzheimer's brain degeneration

J Mackiewicz, M Lisek, T Boczek - Frontiers in Immunology, 2023 - frontiersin.org
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by a progressive
loss of cognitive functions. While the exact causes of this debilitating disorder remain …

[HTML][HTML] Intramolecular activation of strong Si–O bonds by gold (i): regioselective synthesis of 3-bromo-2-silylbenzofurans

P Fernández-Canelas, R Miguélez, E Rubio… - Chemical …, 2022 - pubs.rsc.org
The high reactivity of gold-vinylidene complexes, generated in situ by [1, 2]-bromine shift
from the corresponding 1-bromoalkynes, allows the activation of one of the strongest bonds …

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

F Jiménez-Altayó, A Cabrera, A Bagan… - 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] 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 …

Visualizing reactive astrocytes: Positron emission tomography imaging ligands for imidazoline‐2 binding sites

W Li, Y Qiao, J Chen, Y Li, X Du, SH Liang, H Fu - View, 2023 - Wiley Online Library
Abstract Imidazoline‐2 binding sites (I2BS) exhibit specific expression in reactive astrocytes
of the brain and are implicated in various pathophysiological processes, including …

[HTML][HTML] 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 …

The hyperthermic response to intra-preoptic area administration of agmatine in male rats

J Xu, W Gao, T He, L Yao, H Wu, Z Chen, Y Lai… - Journal of Thermal …, 2023 - Elsevier
Agmatine is an endogenous biogenic amine that exerts various effects on the central
nervous system. The hypothalamic preoptic area (POA, thermoregulatory command center) …

[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 …

[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 …