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 . .