Medicinal Chemistry for Unmet Medical Needs

Unit of Medicinal Chemistry Department of Pharmacology, Toxicology and Therapeutic Chemistry Faculty of Pharmacy and Food Sciences

Unit of Medicinal Chemistry
Department of Pharmacology, Toxicology and Therapeutic Chemistry
Faculty of Pharmacy and Food Sciences

Carmen Escolano Mirón
cescolano@ub.edu
Tel. 934024540

Av. Joan XXIII 27-31 08028 Barcelona

WebSite Group

Principal investigator: Carmen Escolano Mirón   

PhD student: Sergio Rodríguez-Arévalo • Andrea Bagán Polonio

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Current
Research

Our research group, based in the Unit of Medicinal Chemistry at the Faculty of Pharmacy and Food Sciences, is well equipped for all aspects of Medicinal Chemistry. Our team has a multidisciplinary character and is aimed to face projects within chemistry and biology. We are involved in the design and synthesis of organic entities to be used as pharmacological tools for the discovery of molecular mechanisms of action. We are also developing new chemical entities that face health problems with high social impact. In particular, in unmet medical needs such as cancer and neurodegenerative diseases (Alzheimer Disease, AD).

We are currently dedicating our synthetic efforts to two main pipelines of new chemical entities. One is focused on the design and synthesis of mitochondrial PEPCK inhibitors in collaboration with Dr. José Carlos (UB) and Dr. F. Javier Luque (UB). The goal is to unravel the key role of PEPCK in cancer and the development of new chemical tools to be included in the arsenal of strategies for cancer therapeutics.

The other main project is the study of structurally new imidazoline I2 receptor (I2-IR) ligands for the treatment of neurodegenerative diseases. In particular, we have discovered three new families of compounds that show high affinity and selectivity in human brain I2-IR. One lead improved the behavior and cognition in two murine models of neurodegeneration and AD. Thus, we are devoted to propose I2-IR as new target for AD. The project involves recognized pharmacologists: Mercè Pallàs (UB), Luis F. Callado (UPV), J. A. García-Sevilla and J. García-Fuster (UIB), Belén Pérez (UAB). The project leading to these results has received funding from “la Caixa” Foundation, under agreement CI18-00002: I2-Novel compounds for the treatment of neurodegenerative diseases. This activity has received funding from the European Institute of Innovation and Technology (EIT). This body of the European Union receives support from the European Union’s Horizon 2020 research and innovation programme.

Additionally, we regularly collaborate with different academic groups that requests new chemical entities to support/develop their projects. Finally, we have a long tradition providing a wide range of services to different pharmaceutical companies and biotechs, e.g. synthesis of new products; identification, isolation and synthesis of impurities, etc.

Selected
Publications

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.; Djikic, T.; Nikolic, K.; Pallàs, M.; Callado, L. F. and Escolano, C. Bicyclic α‑Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer’s Disease, Journal of Medicinal Chemistry  2020637, 3610-3633, DOI:10.1021/acs.jmedchem.9b02080.

Aragò, M.; Moreno-Felici, J.; Abás, S.; Rodríguez-Arévalo, S; Hyrossova, P.; Figueras, A.; Viñals, F., Pérez, B.; Loza, M. I.; Brea, J.; Latorre, P.; Carrodeguas, J.; García-Roves, P. M.; Galdeano, c.; Ginex, T.; Luque, F. J.; Escolano, C.; Perales, J. C. Pharmacology and preclínica validation of a novel anticancer compound targeting PEPCK-M. Biomedicine and Pharmacotherapy, 121, 2020, 109601, https://doi.org/10.1016/j.biopha.2019.109601

Escolano, C.; Pallàs, M.; Griñán, C.; Abàs, S.; Callado, L.F. García-Sevilla, J. A. SYNTHETIC I2 IMIDAZOLINE RECEPTOR LIGANDS FOR PREVENTION OR TREATMENT OF HUMAN BRAIN DISORDERS. WO/2019/121853

Griñán-Ferré, C.; Vasilopoulou, F.; Abàs, S.; Rodríguez-Arévalo, S.; Bagán, A; Sureda, F. X.; Pérez, B.; Callado, L. F.; García-Sevilla, J. A.; García-Fuster, M. J.; Escolano, C.; Pallàs, M. behavioral and cognitive improvement induced by novel imidazoline I2 receptor ligands in female SAMP8. Neurotherapeutics, 2019, 16(2), 416-431. doi: 10.1007/s13311-018-00681-5

Abas, S., Erdozain, A. M.; Keller, B.; Rodríguez-Arévalo, S.; Callado, L. F.; García-Sevilla, J. A.; Escolano, C. Neuroprotective effects of a structurally new family of high affinity imidazoline I2 receptor ligands. ACS Chem. Neurosci. 8 (4): 737-742, 2017 doi: 10.1021/acschemneuro.6b00426

 

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