ArticleJournal of medicinal chemistry2022
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.
Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 18 citations in OpenAlex.
- Topliss-Guided Optimization of Acetanilide-Based Soluble Epoxide Hydrolase Inhibitors: Exploring the Pentafluorosulfanyl Group as a Potency-Enhancing Motif.ChemMedChem · 2026Article
- Pathophysiology and multi-target prevention strategies for cyclophosphamide-induced bladder injury.iScience · 2026Review
- Activation of anti-inflammatory pathways by polyunsaturated fatty acid signaling may protect neurodevelopment in children prenatally exposed to methylmercury.Environmental health : a global access science source · 2026Article
- Synthesis and optical resolution of 4,5-diaminohomoadamantane: a promising scaffold for chiral ligands and bioactive compounds.Beilstein journal of organic chemistry · 2026Article
- Dimethoxybenzohomoadamantane-based soluble epoxide hydrolase inhibitors:Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Latest developments in small molecule analgesics: heterocyclic scaffolds II.Future medicinal chemistry · 2025Review
- A polycyclic scaffold identified by structure-based drug design effectively inhibits the human P2X7 receptor.Nature communications · 2025Article
- Microglial pro-inflammatory mechanisms induced by monomeric C-reactive protein are counteracted by soluble epoxide hydrolase inhibitors.International immunopharmacology · 2025Article
- Soluble Epoxide Hydrolase Inhibition Improves Alzheimer's Disease Hallmarks: Correlation with Peripheral Inflammation and Gut Microbiota Modulation.Aging and disease · 2025Article
- Applications of Bridgehead Heterocycles in Drug Design and Medicinal Chemistry.Topics in current chemistry (Cham) · 2025Review
- Electrical Properties of Cu-Based Coordination Complexes: Insights from In Situ Impedance Spectroscopy.Molecules (Basel, Switzerland) · 2024Article
- Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.Journal of medicinal chemistry · 2024Article
Corrections and comments
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Authors and funding
23 authors at 11 institutions in 4 countries.
Funding
Abstract
The soluble epoxide hydrolase (sEH) has been suggested as a pharmacological target for the treatment of several diseases, including pain-related disorders. Herein, we report further medicinal chemistry around new benzohomoadamantane-based sEH inhibitors (sEHI) in order to improve the drug metabolism and pharmacokinetics properties of a previous hit. After an extensive in vitro screening cascade, molecular modeling, and in vivo pharmacokinetics studies, two candidates were evaluated in vivo in a murine model of capsaicin-induced allodynia. The two compounds showed an anti-allodynic effect in a dose-dependent manner. Moreover, the most potent compound presented robust analgesic efficacy in the cyclophosphamide-induced murine model of cystitis, a well-established model of visceral pain. Overall, these results suggest painful bladder syndrome as a new possible indication for sEHI, opening a new range of applications for them in the visceral pain field.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.