TY  - JOUR
AU  - Abás, Sònia
AU  - Rodríguez-Arévalo, Sergio
AU  - Bagán, Andrea
AU  - Griñán-Ferré, Christian
AU  - Vasilopoulou, Foteini
AU  - Brocos-Mosquera, Iria
AU  - Muguruza, Carolina
AU  - Pérez, Belén
AU  - Molins, Elies
AU  - Luque, F. Javier
AU  - Pérez-Lozano, Pilar
AU  - De Jonghe, Steven
AU  - Daelemans, Dirk
AU  - Naesens, Lieve
AU  - Brea, José
AU  - Loza, M. Isabel
AU  - Hernández-Hernández, Elena
AU  - García-Sevilla, Jesús A.
AU  - García-Fuster, M. Julia
AU  - Radan, Milica
AU  - Đikić, Teodora
AU  - Nikolić, Katarina
AU  - Pallàs, Mercè
AU  - Callado, Luis F.
AU  - Escolano, Carmen
PY  - 2020
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3768
AB  - Page 3630. The affiliation of the following authors needs to be corrected. Iria Brocos-Mosquera is affiliated with Department of Pharmacology, University of the Basque Country, UPV/ EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigacioìn Biomeìdica en Red de Salud Mental, CIBERSAM, Spain. Carolina Muguruza is affiliated with Department of Pharmacology, University of the Basque Country, UPV/ EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigacioìn Biomeìdica en Red de Salud Mental, CIBERSAM, Spain. Luis F. Callado is affiliated with Department of Pharmacology, University of the Basque Country, UPV/EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigacioìn Biomeìdica en Red de Salud Mental, CIBERSAM, Spain.
PB  - American Chemical Society
T2  - Journal of Medicinal Chemistry
T1  - Erratum: Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2Receptor Ligands for Alzheimer's Disease (Journal of Medicinal Chemistry (2020) 63:7 (3610−3633) DOI: 10.1021/acs.jmedchem.9b02080)
VL  - 63
IS  - 18
SP  - 10529
DO  - 10.1021/acs.jmedchem.0c01324
ER  - 

@article{
author = "Abás, Sònia and Rodríguez-Arévalo, Sergio and Bagán, Andrea and Griñán-Ferré, Christian and Vasilopoulou, Foteini and Brocos-Mosquera, Iria and Muguruza, Carolina and Pérez, Belén and Molins, Elies and Luque, F. Javier and Pérez-Lozano, Pilar and De Jonghe, Steven and Daelemans, Dirk and Naesens, Lieve and Brea, José and Loza, M. Isabel and Hernández-Hernández, Elena and García-Sevilla, Jesús A. and García-Fuster, M. Julia and Radan, Milica and Đikić, Teodora and Nikolić, Katarina and Pallàs, Mercè and Callado, Luis F. and Escolano, Carmen",
year = "2020",
abstract = "Page 3630. The affiliation of the following authors needs to be corrected. Iria Brocos-Mosquera is affiliated with Department of Pharmacology, University of the Basque Country, UPV/ EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigacioìn Biomeìdica en Red de Salud Mental, CIBERSAM, Spain. Carolina Muguruza is affiliated with Department of Pharmacology, University of the Basque Country, UPV/ EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigacioìn Biomeìdica en Red de Salud Mental, CIBERSAM, Spain. Luis F. Callado is affiliated with Department of Pharmacology, University of the Basque Country, UPV/EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigacioìn Biomeìdica en Red de Salud Mental, CIBERSAM, Spain.",
publisher = "American Chemical Society",
journal = "Journal of Medicinal Chemistry",
title = "Erratum: Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2Receptor Ligands for Alzheimer's Disease (Journal of Medicinal Chemistry (2020) 63:7 (3610−3633) DOI: 10.1021/acs.jmedchem.9b02080)",
volume = "63",
number = "18",
pages = "10529",
doi = "10.1021/acs.jmedchem.0c01324"
}

Abás, S., Rodríguez-Arévalo, S., Bagán, A., Griñán-Ferré, C., Vasilopoulou, F., Brocos-Mosquera, I., Muguruza, C., Pérez, B., Molins, E., Luque, F. J., Pérez-Lozano, P., De Jonghe, S., Daelemans, D., Naesens, L., Brea, J., Loza, M. I., Hernández-Hernández, E., García-Sevilla, J. A., García-Fuster, M. J., Radan, M., Đikić, T., Nikolić, K., Pallàs, M., Callado, L. F.,& Escolano, C.. (2020). Erratum: Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2Receptor Ligands for Alzheimer's Disease (Journal of Medicinal Chemistry (2020) 63:7 (3610−3633) DOI: 10.1021/acs.jmedchem.9b02080). in Journal of Medicinal Chemistry
American Chemical Society., 63(18), 10529.
https://doi.org/10.1021/acs.jmedchem.0c01324

Abás S, Rodríguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez-Lozano P, De Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernández-Hernández E, García-Sevilla JA, García-Fuster MJ, Radan M, Đikić T, Nikolić K, Pallàs M, Callado LF, Escolano C. Erratum: Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2Receptor Ligands for Alzheimer's Disease (Journal of Medicinal Chemistry (2020) 63:7 (3610−3633) DOI: 10.1021/acs.jmedchem.9b02080). in Journal of Medicinal Chemistry. 2020;63(18):10529.
doi:10.1021/acs.jmedchem.0c01324 .

Abás, Sònia, Rodríguez-Arévalo, Sergio, Bagán, Andrea, Griñán-Ferré, Christian, Vasilopoulou, Foteini, Brocos-Mosquera, Iria, Muguruza, Carolina, Pérez, Belén, Molins, Elies, Luque, F. Javier, Pérez-Lozano, Pilar, De Jonghe, Steven, Daelemans, Dirk, Naesens, Lieve, Brea, José, Loza, M. Isabel, Hernández-Hernández, Elena, García-Sevilla, Jesús A., García-Fuster, M. Julia, Radan, Milica, Đikić, Teodora, Nikolić, Katarina, Pallàs, Mercè, Callado, Luis F., Escolano, Carmen, "Erratum: Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2Receptor Ligands for Alzheimer's Disease (Journal of Medicinal Chemistry (2020) 63:7 (3610−3633) DOI: 10.1021/acs.jmedchem.9b02080)" in Journal of Medicinal Chemistry, 63, no. 18 (2020):10529,
https://doi.org/10.1021/acs.jmedchem.0c01324 . .

TY  - JOUR
AU  - Abás, Sònia
AU  - Rodríguez-Arévalo, Sergio
AU  - Bagán, Andrea
AU  - Griñán-Ferré, Christian
AU  - Vasilopoulou, Foteini
AU  - Brocos-Mosquera, Iria
AU  - Muguruza, Carolina
AU  - Pérez, Belén
AU  - Molins, Elies
AU  - Luque, F. Javier
AU  - Pérez-Lozano, Pilar
AU  - De Jonghe, Steven
AU  - Daelemans, Dirk
AU  - Naesens, Lieve
AU  - Brea, José
AU  - Loza, M. Isabel
AU  - Hernández-Hernández, Elena
AU  - García-Sevilla, Jesús A.
AU  - García-Fuster, M. Julia
AU  - Radan, Milica
AU  - Đikić, Teodora
AU  - Nikolić, Katarina
AU  - Pallàs, Mercè
AU  - Callado, Luis F.
AU  - Escolano, Carmen
PY  - 2020
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3576
AB  - 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 new I2-IR ligands are urgently required for improving their pharmacological characterization. We report the synthesis and three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of a new family of bicyclic α-iminophosphonates endowed with relevant affinities for human brain I2-IR. Acute treatment in mice with a selected compound significantly decreased Fas-associated protein with death domain (FADD) in the hippocampus, a key signaling mediator of neuroprotective actions. Additionally, in vivo studies in the familial Alzheimer's disease 5xFAD murine model revealed beneficial effects in behavior and cognition. These results are supported by changes in molecular pathways related to cognitive decline and Alzheimer's disease. Therefore, bicyclic α-iminophosphonates are tools that may open new therapeutic avenues for I2-IR, particularly for unmet neurodegenerative conditions.
PB  - American Chemical Society
T2  - Journal of Medicinal Chemistry
T1  - Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease
VL  - 63
IS  - 7
SP  - 3610
EP  - 3633
DO  - 10.1021/acs.jmedchem.9b02080
ER  - 

@article{
author = "Abás, Sònia and Rodríguez-Arévalo, Sergio and Bagán, Andrea and Griñán-Ferré, Christian and Vasilopoulou, Foteini and Brocos-Mosquera, Iria and Muguruza, Carolina and Pérez, Belén and Molins, Elies and Luque, F. Javier and Pérez-Lozano, Pilar and De Jonghe, Steven and Daelemans, Dirk and Naesens, Lieve and Brea, José and Loza, M. Isabel and Hernández-Hernández, Elena and García-Sevilla, Jesús A. and García-Fuster, M. Julia and Radan, Milica and Đikić, Teodora and Nikolić, Katarina and Pallàs, Mercè and Callado, Luis F. and Escolano, Carmen",
year = "2020",
abstract = "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 new I2-IR ligands are urgently required for improving their pharmacological characterization. We report the synthesis and three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of a new family of bicyclic α-iminophosphonates endowed with relevant affinities for human brain I2-IR. Acute treatment in mice with a selected compound significantly decreased Fas-associated protein with death domain (FADD) in the hippocampus, a key signaling mediator of neuroprotective actions. Additionally, in vivo studies in the familial Alzheimer's disease 5xFAD murine model revealed beneficial effects in behavior and cognition. These results are supported by changes in molecular pathways related to cognitive decline and Alzheimer's disease. Therefore, bicyclic α-iminophosphonates are tools that may open new therapeutic avenues for I2-IR, particularly for unmet neurodegenerative conditions.",
publisher = "American Chemical Society",
journal = "Journal of Medicinal Chemistry",
title = "Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease",
volume = "63",
number = "7",
pages = "3610-3633",
doi = "10.1021/acs.jmedchem.9b02080"
}

Abás, S., Rodríguez-Arévalo, S., Bagán, A., Griñán-Ferré, C., Vasilopoulou, F., Brocos-Mosquera, I., Muguruza, C., Pérez, B., Molins, E., Luque, F. J., Pérez-Lozano, P., De Jonghe, S., Daelemans, D., Naesens, L., Brea, J., Loza, M. I., Hernández-Hernández, E., García-Sevilla, J. A., García-Fuster, M. J., Radan, M., Đikić, T., Nikolić, K., Pallàs, M., Callado, L. F.,& Escolano, C.. (2020). Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease. in Journal of Medicinal Chemistry
American Chemical Society., 63(7), 3610-3633.
https://doi.org/10.1021/acs.jmedchem.9b02080

Abás S, Rodríguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez-Lozano P, De Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernández-Hernández E, García-Sevilla JA, García-Fuster MJ, Radan M, Đikić T, Nikolić K, Pallàs M, Callado LF, Escolano C. Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease. in Journal of Medicinal Chemistry. 2020;63(7):3610-3633.
doi:10.1021/acs.jmedchem.9b02080 .

Abás, Sònia, Rodríguez-Arévalo, Sergio, Bagán, Andrea, Griñán-Ferré, Christian, Vasilopoulou, Foteini, Brocos-Mosquera, Iria, Muguruza, Carolina, Pérez, Belén, Molins, Elies, Luque, F. Javier, Pérez-Lozano, Pilar, De Jonghe, Steven, Daelemans, Dirk, Naesens, Lieve, Brea, José, Loza, M. Isabel, Hernández-Hernández, Elena, García-Sevilla, Jesús A., García-Fuster, M. Julia, Radan, Milica, Đikić, Teodora, Nikolić, Katarina, Pallàs, Mercè, Callado, Luis F., Escolano, Carmen, "Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease" in Journal of Medicinal Chemistry, 63, no. 7 (2020):3610-3633,
https://doi.org/10.1021/acs.jmedchem.9b02080 . .

TY  - CONF
AU  - Bagán, Andrea
AU  - Abás, Sònia
AU  - Rodríguez-Arévalo, Sergio
AU  - Rodríguez-Arévalo, Gemma
AU  - Vasilopoulou, Fotini
AU  - Griñán-Ferré, Christian
AU  - Pallàs, Mercè
AU  - Pérez-Lozano, Pilar
AU  - Radan, Milica
AU  - Đikić, Teodora
AU  - Nikolić, Katarina
AU  - Escolano, Carmen
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4892
AB  - 2-Imidazoline-containing compounds constitute a valuable class of agents that modulate α2-
adrenergic receptors and often show a high affinity for imidazoline I2-receptors (I2-IR). Moreover, 2-
imidazolines are an important class of heterocyclic scaffolds found in natural product chemistry,
coordination chemistry, and homogeneous catalysis. To meet the demand for 2-imidazolinecontaining
compounds, different synthetic approximations were developed. In this work, we
describe an efficient and user-friendly synthetic process involving the combination of isocyanidebased
multicomponent reaction and microwave heating without the need of anhydrous atmosphere
or additional solvents that generates unprecedented (2-imidazolin-4-yl)phosphonates [1].
We assessed the pharmacological profile and selectivity of the prepared compounds upon I2-IR.
Owing to the outstanding high I2-IR affinity of one of the prepared compounds and high selectivity
devoid to the α2-adrenoceptor of other compounds, markedly better than any described I2-IR ligand
to date, (2-imidazolin-4-yl)phosphonates might be considered as a suitable scaffold for designing
novel I2-IR ligands [2]. In addition, we demonstrated the effectiveness of two of the new I2-IR ligands
in an in vivo female model for cognitive decline (SAMP8), and we analyzed the pathological
biomarkers for neurodegeneration. This study is the first experimental evidence that demonstrates
the possibility of using this receptor as a target for cognitive impairment [3].
Note, theoretical studies were carried out for designing compounds with enhanced activity and
selectivity upon I2-IR based on created 3D-QSAR model.
In this work, green chemistry to access an unprecedented scaffold and promising pharmacological
results in the neurodegeneration field walked together.
PB  - MDPI
C3  - Proceedings
T1  - (2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together
VL  - 22
IS  - 1
DO  - 10.3390/proceedings2019022097
ER  - 

@conference{
author = "Bagán, Andrea and Abás, Sònia and Rodríguez-Arévalo, Sergio and Rodríguez-Arévalo, Gemma and Vasilopoulou, Fotini and Griñán-Ferré, Christian and Pallàs, Mercè and Pérez-Lozano, Pilar and Radan, Milica and Đikić, Teodora and Nikolić, Katarina and Escolano, Carmen",
year = "2019",
abstract = "2-Imidazoline-containing compounds constitute a valuable class of agents that modulate α2-
adrenergic receptors and often show a high affinity for imidazoline I2-receptors (I2-IR). Moreover, 2-
imidazolines are an important class of heterocyclic scaffolds found in natural product chemistry,
coordination chemistry, and homogeneous catalysis. To meet the demand for 2-imidazolinecontaining
compounds, different synthetic approximations were developed. In this work, we
describe an efficient and user-friendly synthetic process involving the combination of isocyanidebased
multicomponent reaction and microwave heating without the need of anhydrous atmosphere
or additional solvents that generates unprecedented (2-imidazolin-4-yl)phosphonates [1].
We assessed the pharmacological profile and selectivity of the prepared compounds upon I2-IR.
Owing to the outstanding high I2-IR affinity of one of the prepared compounds and high selectivity
devoid to the α2-adrenoceptor of other compounds, markedly better than any described I2-IR ligand
to date, (2-imidazolin-4-yl)phosphonates might be considered as a suitable scaffold for designing
novel I2-IR ligands [2]. In addition, we demonstrated the effectiveness of two of the new I2-IR ligands
in an in vivo female model for cognitive decline (SAMP8), and we analyzed the pathological
biomarkers for neurodegeneration. This study is the first experimental evidence that demonstrates
the possibility of using this receptor as a target for cognitive impairment [3].
Note, theoretical studies were carried out for designing compounds with enhanced activity and
selectivity upon I2-IR based on created 3D-QSAR model.
In this work, green chemistry to access an unprecedented scaffold and promising pharmacological
results in the neurodegeneration field walked together.",
publisher = "MDPI",
journal = "Proceedings",
title = "(2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together",
volume = "22",
number = "1",
doi = "10.3390/proceedings2019022097"
}

Bagán, A., Abás, S., Rodríguez-Arévalo, S., Rodríguez-Arévalo, G., Vasilopoulou, F., Griñán-Ferré, C., Pallàs, M., Pérez-Lozano, P., Radan, M., Đikić, T., Nikolić, K.,& Escolano, C.. (2019). (2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together. in Proceedings
MDPI., 22(1).
https://doi.org/10.3390/proceedings2019022097

Bagán A, Abás S, Rodríguez-Arévalo S, Rodríguez-Arévalo G, Vasilopoulou F, Griñán-Ferré C, Pallàs M, Pérez-Lozano P, Radan M, Đikić T, Nikolić K, Escolano C. (2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together. in Proceedings. 2019;22(1).
doi:10.3390/proceedings2019022097 .

Bagán, Andrea, Abás, Sònia, Rodríguez-Arévalo, Sergio, Rodríguez-Arévalo, Gemma, Vasilopoulou, Fotini, Griñán-Ferré, Christian, Pallàs, Mercè, Pérez-Lozano, Pilar, Radan, Milica, Đikić, Teodora, Nikolić, Katarina, Escolano, Carmen, "(2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together" in Proceedings, 22, no. 1 (2019),
https://doi.org/10.3390/proceedings2019022097 . .