Polycyclic Compounds With Biological Activity

Department of Pharmacology, Toxicology and Therapeutic Chemistry

Faculty of Pharmacy and Food Sciences, UB

Santiago Vázquez
ORCID ID: 0000-0002-9296-6026
Tel +34 934024533
https://www.ub.edu/medicinalchemistrypharmacology/research-group/santiago-vazquez/

Principal investigator: • Santiago Vázquez
Lecturers: • Sandra Codony Gisbert  • Andreea L. Turcu
Assistant Professor: • Eugènia Pujol Bech PostDocs: • Antonino Fallica
PhD students:  • Celia Escriche • Javier Sánchez • Alba López • Giorgio Emmola

Santiago-Vázquez

Current
Research

Our research revolves around the design, synthesis and characterization of new compounds of therapeutic interest. The biological activity of these compounds is evaluated by several collaborators with expertise in each specific biological target. We are particularly interested in:

  1. Antivirals agents, mainly against influenza A virus; in collaboration with the groups of Prof. L. Naesens and Graciela Andrei (Rega Institute for Medical Research, Leuven, Belgium), and Prof. F. J. Luque (IBUB);
  2. NMDA receptor antagonists, of interest in neurodegenerative diseases; in collaboration with Prof. F. X. Sureda (Universitat Rovira i Virgili, Tarragona, Spain), Prof. J. W. Johnson (University of Pittsburgh, USA) and Prof. D. Soto (UB);
  3. Soluble epoxide hydrolase inhibitors, of interest in inflammatory and neurodegenerative diseases; in collaboration with the groups of Prof. M. Pallàs (UB and the Institute of Neuroscience of the UB, UBNeuro) and Dr. C. Morisseau (University of California, Davis, USA).
  4. Sigma-1 receptor antagonists, of interest in analgesia; in collaboration with the group of Prof. Enrique J. Cobos (Univ. Granada).
  5. P2X7 receptor antagonists, of interest in inflammatory and neurodegenerative diseases; in collaboration with Dr. S. E. Mansoor (Oregon Health & Science University, USA), Prof. A. Nicke (Univ. Munich, Germany), Prof. A. Kolocouris (Univ. Athens, Greece), and Prof. C. E. Müller (Univ. Bonn, Germany).

Of note, in addition to our academic interests, we have an excellent track record of collaborations with several chemical and pharmaceutical companies that have led to several patent applications stemmed from join research projects and services.

Within our group, a particular emphasis is placed on providing our PhD students with outstanding training not only in experimental research but also in teaching, scientific writing, communication, and social skills, etc. Six former PhD students were awarded the “Extraordinary Price for PhD of the UB” and two of them were subsequently funded by the prestigious “Marie Curie Fellowship”. We are proud of the prominent positions that the former members of our group currently held in private chemical and pharmaceutical companies or as academics.

Selected
Publications

Oken, A. C.; Turcu, A. L.; Tzortzini E.; Georgiou, K.; Nagel, J.; Westermann, F. G.; Barniol-Xicota, M.; Seidler, J.; Kim, G. R.; Lee, S. D.; Nicke, A.; Kim, Y.-C.; Müller, C. E.; Kolocouris, A.; Vázquez, S.; Mansoor, S. E. A polycyclic scaffold identified by structure-based drug design effectively inhibits the human P2X7 receptor. Nature Communications 16:8283, 2025. doi: 10.1038/s41467-025-62643-8

Codony, S.; Jora, B.; Santos-Caballero, M.; Qiu, Q.; Calvó-Tusell, C.; Escriche, C.; Turcu, A. L.; Prischi, F.; Bartra, C.; Val, C.; Morisseau, C.; Pérez, B.; Bertran-Mostazo, A.; Osuna, S.; Corpas, R.; Griñán-Ferré, C.; Galdeano, C.; Loza, M. I.; Pallàs, M.; Sanfeliu, C; Hammock, B. D.; Brea, J.; Feixas, F.; Conte, M. R.; Cobos, E. J.; Vázquez, S. Dimethoxybenzohomoadamantane-based soluble epoxide hydrolase inhibitors: in vivo efficacy in a murine model of chemotherapy-induced neuropathic pain. Journal of Enzyme Inhibition and Medicinal Chemistry 40:2574990, 2025. doi: 10.1080/14756366.2025.2574990

Rimaux, S.; Valdivia, A.; Martín-López, J.; Francesconi, V.; Escriche, C.; Mestdagh, C.; Van Berwaer, R.; Schurmans, L.; Verleye, K.; Noppen, S.; Lozano, O.; Stevaert, A.; Luque, F. J.; Naesens, L.; Vázquez, S. N-[(Thiophen-3-yl)methyl]benzamides as influenza virus fusion inhibitors acting on H1 and H5 hemagglutinins. Journal of Medicinal Chemistry 68: 18491-18518 , 2025. doi: 10.1021/acs.jmedchem.5c01357

Carrillo, E.; Montaño Romero, A.; González, C. U.; Turcu, A. L.; Vázquez, S.; Twomey, E. C.; Jayaraman, V. Memantine inhibits calcium-permeable AMPA receptors. Nature Communications 16:5576, 2025. doi: 10.1038/s41467-025-60543-5

Van Loy, B.; Pujol, E.; Kamata, K.; Lee, X.Y.; Bakirtzoglou, N.; Van Berwaer, R.; Vandeput, J.; Mestdagh, C.; Persoons, L.; De Wijngaert, B.; Goovaerts, Q.; Noppen, S.; Jacquemyn, M.; Ahmadzadeh, K.; Bernaerts, E.; Martín-López, J.; Escriche, C.; Vanmechelen, B.; Krasniqi, B.; Singh, A. K.; Daelemans, D.; Maes, P.; Matthys, P.; Dehaen, W.; Rozenski, J.; Das, K.; Voet, A.; Vázquez, S.; Naesens, L.; Stevaert, A. A guanidine-based coronavirus replication inhibitor which targets the nsp15 endoribonuclease and selects for interferon-susceptible mutant viruses. PLoS Pathogens 21:e1012571, 2025. doi: 10.1371/journal.ppat.1012571

Selected
Publications

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Author

Identification

Pérez-Areales, F. J.; Turcu, A. L.; Barniol-Xicota, M.; Pont, C.; Pivetta, D.; Espargaró, A.; Bartolini, M.; De Simone, A.; Andrisano, V.; Pérez, B.; Sabate, R.; Sureda, F. X.; Vázquez, S.; Muñoz-Torrero, D. A novel class of multitarget anti-Alzheimer benzohomoadamantane chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. Eur. J. Med. Chem. 180:613-626, 2019. doi: 10.1016/j.ejmech.2019.07.051

 

Leiva, R.; Phillips, M. B.; Turcu, A. L.; Gratacòs-Batlle, E.; León-García, L. ; Sureda, F. X.; Soto, D.; Johnson, J. W.; Vázquez, S. Pharmacological and electrophysiological characterization of novel NMDA receptor antagonists. ACS Chem. Neurosci. 9:2722-2730, 2018. doi: 10.1021/acschemneuro.8b00154

 

Leiva, R.; Barniol-Xicota, M.; Codony, S.; Ginex, T.; Vanderlinden, E.; Montes, M.; Caffrey, M.; Luque, F. J.; Naesens, L.; Vázquez, S. Aniline-based inhibitors of influenza H1N1 virus acting on hemagglutinin-mediated fusion. J. Med. Chem. 61:98-118, 2018. doi: 10.1021/acs.jmedchem.7b00908

 

Leiva, R.; Griñan-Ferré, C.; Seira, C.; Valverde, E.; McBride, A.; Binnie, M.; Pérez, B.; Luque, F. J.; Pallàs, M.; Bidon-Chanal, A.; Webster, S. P.; Vázquez, S. Design, synthesis and in vivo study of novel pyrrolidine-based 11b-HSD1 inhibitors for age-related cognitive dysfunction. Eur. J. Med. Chem. 139:412-428, 2017. doi: 10.1016/j.ejmech.2017.08.003

 

Barniol-Xicota, M.; Gazzarrini, S.; Torres, E.; Hu, Y.; Wang, J.; Naesens, L.; Moroni, A.; Vázquez, S. Slow but steady wins the race: dissimilarities among new dual inhibitors of the wild-type and the V27A mutant M2 channels of influenza A virus. J. Med. Chem. 60:3727-3738, 2017. doi: 10.1021/acs.jmedchem.6b01758

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