Design, synthesis and evaluation of novel soluble epoxide hydrolase (sEH) inhibitors for inflammatory diseases.

This is a more recent topic within our group. We have recently discovered that the lipophilic cavity of the sEH is big enough for accommodating very large lipophilic units, such as that the diamantane (a). We have also discovery a few new families of very potent sEH inhibitors endowed with interesting DMPK properties (b). This project is in collaboration with the groups of Prof. Bruce D. Hammock and Christophe Morisseau (University of California Davis, Davis, USA), Prof. Manuel Vázquez-Carrera and Prof. Mercè Pallàs (UB), and Prof. Mabel Loza and José M. Brea (Universidad de Santiago de Compostela, Spain).

  • Codony, S.; Valverde, E.; Leiva, R.; Brea, J.; Loza, M. I.; Morisseau, C.; Hammock, B. D.; Vázquez, S. Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors. Bioorg. Med. Chem. 2019, 27, 115078.
  • Griñán-Ferré, C.; Codony, S.; Pujol, E.; Yang, J.; Leiva, R.; Escolano, C.; Puigoriol-Illamola, D.; Companys-Alemany, J.; Corpas, R.; Sanfeliu, C.; Pérez, B.; Loza, M. I.; Brea, J.; Morisseau, C.; Hammock, B. D.; Vázquez, S.; Pallàs, M.; Galdeano, C.Pharmacological Inhibition of Soluble Epoxide Hydrolase as a New Therapy for Alzheimer’s Disease. Neurotherapeutics, 2020, 17, 1825-1835.
  • Codony, S.; Pujol, E.; Pizarro, J.; Feixas, F.; Valverde, E.; Loza, M. I.; Brea, J. M.; Saez, E.; Oyarzabal, J.; Pineda-Lucena, A.; Pérez, B.; Pérez, C.; Rodríguez-Franco, M. I.; Leiva, R.; Osuna, S.; Morisseau, C.; Hammock, B. D.; Vázquez-Carrera, M.; Vázquez, S. 2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: In Vivo Evaluation in a Murine Model of Acute Pancreatitis. J. Med. Chem.63, 9237–9257.
  • Martín-López, J.; Codony, S.; Bartra, C.; Morisseau, C.; Loza, M. I.; Sanfeliu, C.; Hammock, B. D.; Brea, J.; Vázquez, S. (Piperidin-4-yl)acetamides as Potent Inhibitors of Soluble Epoxide Hydrolase with Anti-Inflammatory Activity. Pharmaceuticals, 2021,  14, 1323.
  • Codony, S.; Calvó-Tusell, C.; Valverde, E.; Osuna, S.; Morisseau, C.; Loza, M. I.; Brea, J.; Pérez, C.; Rodríguez-Franco, M. I.; Pizarro-Delgado, J.; Corpas, R.; Griñán-Ferré, C.; Pallàs, M.; Sanfeliu, C.; Vázquez-Carrera, M.; Hammock, B. D.; Feixas, F.; Vázquez, S. From the Design to the In Vivo Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis. J. Med. Chem., 2021, 64, 5429–5446.

Diagnostics with Modern Chemical Probes

Generation of functional probes by modern chemistry such as CH activation for modified tryptophan peptides and the preparation of fluorescent…

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Neurodegeneration in ageing and neurodegenerative diseases

 We focus our research in the study of the molecular mechanisms involved in behavioral abnormalities and cognitive decline, by using…

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Design, synthesis and evaluation of new polycyclic inhibitors of the M2 channel of the influenza A virus.

Amantadine and rimantadine have been in clinical use as anti-influenza A virus agents for decades. The mechanism of action of…

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New imidazoline I2 receptor ligands

The imidazoline I2 receptors (I2-IRs) are altered in the brain of Alzheimer’s disease patients and I2-IR ligands may have therapeutic…

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