2-(Piperidin-4-yl)acetamides as Potent Inhibitors of Soluble Epoxide Hydrolase with Anti-Inflammatory Activity

Martín-López, J.; Codony, S.; Bartra, C.; Morisseau, C.; Loza, M.I.; Sanfeliu, C.; Hammock, B.D.; Brea, J.; Vázquez, S. Pharmaceuticals, 2021, 14, 1323.

The pharmacological inhibition of soluble epoxide hydrolase (sEH) has been suggested as a potential therapy for the treatment of pain and inflammatory diseases through the stabilization of endogenous epoxyeicosatrienoic acids. Numerous potent sEH inhibitors (sEHI) have been developed, however many contain highly lipophilic substituents limiting their availability. Recently, a new series of benzohomoadamantane-based ureas endowed with potent inhibitory activity for the human and murine sEH was reported. However, their very low microsomal stability prevented further development. Herein, a new series of benzohomoadamantane-based amides were synthetized, fully characterized, and evaluated as sEHI. Most of these amides were endowed with excellent inhibitory potencies. A selected compound displayed anti-inflammatory effects with higher effectiveness than the reference sEHI, TPPU.

Unveiling the multitarget anti-Alzheimer drug discovery landscape: A bibliometric analysis

Sampietro, A.; Pérez-Areales, F. J.; Martínez, P.; Arce, E. M.; Galdeano, C.; Muñoz-Torrero, D. Pharmaceuticals 2022, 15, 545

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Discovery and in vivo proof of concept of a highly potent dual inhibitor of soluble epoxide hydrolase and acetylcholinesterase for the treatment of Alzheimer’s disease

Codony, S.; Pont, C.; Griñán-Ferré, C.; Di Pede-Mattatelli, A.; Calvó-Tusell, C.; Feixas, F.; Osuna, S.; Jarné-Ferrer, J.; Naldi, M.; Bartolini,…

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Disease-modifying treatment with I 2 imidazoline receptor ligand LSL60101 in an Alzheimer’s disease mouse model: a comparative study with donepezil

Vasilopoulou F, Rodríguez-Arévalo S, Bagán A, Escolano C, Griñán-Ferré C, Pallàs M. Disease-modifying treatment with I2 imidazoline receptor ligand LSL60101 in…

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Inhibition of Soluble Epoxide Hydrolase Ameliorates Phenotype and Cognitive Abilities in a Murine Model of Niemann Pick Type C Disease

Griñán-Ferré C, Companys-Alemany J, Jarné-Ferrer J, Codony S, González-Castillo C, Ortuño-Sahagún D, Vilageliu L, Grinberg D, Vázquez S, Pallàs M.…

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A Novel NMDA Receptor Antagonist Protects against Cognitive Decline Presented by Senescent Mice.

Companys-Alemany J, Turcu AL, Bellver-Sanchis A, Loza MI, Brea JM, Canudas AM, Leiva R, Vázquez S, Pallàs M, Griñán-Ferré C.Pharmaceutics. 2020. 12(3). pii: E284. doi: 10.3390/pharmaceutics12030284. https://www.mdpi.com/1999-4923/12/3/284/htm

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