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cc-by (c) Martín López, Juan et al., 2021
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/194120

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

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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. Keywords: DMPK properties; amide; benzohomoadamantane; piperidine; soluble epoxide hydrolase.

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MARTÍN LÓPEZ, Juan, et al. 2-(Piperidin-4-yl)acetamides as Potent Inhibitors of Soluble Epoxide Hydrolase with Anti-Inflammatory Activity. Pharmaceuticals. 2021. Vol. 14, num. 12. ISSN 1424-8247. [consulted: 9 of August of 2026]. Available at: https://hdl.handle.net/2445/194120

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