(2-Imidazolin-4-yl)phosphonates: Green Chemistry and Biology Walk Together
Аутори
Bagán, AndreaAbás, 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
Конференцијски прилог (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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.
Извор:
Proceedings, 2019, 22, 1Издавач:
- MDPI
Финансирање / пројекти:
- Синтеза, квантитативни однос између структуре и дејства, физичко-хемијска карактеризација и анализа фармаколошки активних супстанци (RS-MESTD-Basic Research (BR or ON)-172033)
Напомена:
- The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019
Институција/група
PharmacyTY - 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 . .