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View article: Dimethoxybenzohomoadamantane-based soluble epoxide hydrolase inhibitors: <i>in vivo</i> efficacy in a murine model of chemotherapy-induced neuropathic pain
Dimethoxybenzohomoadamantane-based soluble epoxide hydrolase inhibitors: <i>in vivo</i> efficacy in a murine model of chemotherapy-induced neuropathic pain Open
The soluble epoxide hydrolase (sEH) has recently emerged as a promising target for the treatment of several pain-related conditions. Herein, we report the design and synthesis of a peripherally restricted sEH inhibitor with high potency an…
View article: Idler Compounds: A Simple Protocol for Openly Sharing Fridge Contents for Cross-Screening
Idler Compounds: A Simple Protocol for Openly Sharing Fridge Contents for Cross-Screening Open
The first step in discovering novel medicines is identifying an initial hit against a biological target or organism, followed by extensive iterative processes to explore the structure-activity relationship and establish a lead compound. As…
View article: Microglial pro-inflammatory mechanisms induced by monomeric C-reactive protein are counteracted by soluble epoxide hydrolase inhibitors
Microglial pro-inflammatory mechanisms induced by monomeric C-reactive protein are counteracted by soluble epoxide hydrolase inhibitors Open
View article: Polycyclic compounds as soluble epoxide hydrolase inhibitors
Polycyclic compounds as soluble epoxide hydrolase inhibitors Open
View article: Novel Soluble Epoxide Hydrolase Inhibitor: Toward Regulatory Preclinical Studies
Novel Soluble Epoxide Hydrolase Inhibitor: Toward Regulatory Preclinical Studies Open
Neuroinflammation is widely recognized as a key pathological hallmark of Alzheimer's disease (AD). Recently, inhibiting soluble epoxide hydrolase (sEH) has emerged as a promising therapeutic strategy for AD. sEH plays a pivotal role in neu…
View article: Soluble Epoxide Hydrolase Inhibition Improves Alzheimer’s Disease Hallmarks: Correlation with Peripheral Inflammation and Gut Microbiota Modulation
Soluble Epoxide Hydrolase Inhibition Improves Alzheimer’s Disease Hallmarks: Correlation with Peripheral Inflammation and Gut Microbiota Modulation Open
Targeting brain inflammation has been proposed as a promising therapeutic strategy to cope with neurodegenerative diseases. Interestingly, accumulating data suggest that the gut microbiota partially exerts its neurodegenerative effects by …
View article: Novel molecular mechanism driving neuroprotection after soluble epoxide hydrolase inhibition: Insights for Alzheimer's disease therapeutics
Novel molecular mechanism driving neuroprotection after soluble epoxide hydrolase inhibition: Insights for Alzheimer's disease therapeutics Open
Background Neuroinflammation is widely recognized as a significant hallmark of Alzheimer's disease (AD). To combat neuroinflammation, the inhibition of the soluble epoxide hydrolase (sEH) enzyme has been demonstrated crucial. Importantly, …
View article: Soluble epoxide hydrolase inhibitors counteract microglia pro-inflammatory response induced by monomeric C-reactive protein
Soluble epoxide hydrolase inhibitors counteract microglia pro-inflammatory response induced by monomeric C-reactive protein Open
Neuroinflammation is a crucial neuropathological trait in Alzheimer’s disease (AD), although its role in the development of AD is not clarified. We previously proposed the monomeric C-reactive protein (mCRP), which is generated by activati…
View article: An Optimized Soluble Epoxide Inhibitor Unveils Changes in Novel Molecular Mechanism Driving Neuroprotection in Alzheimer's Disease in <i>in vitro</i> and <i>in vivo</i> Models
An Optimized Soluble Epoxide Inhibitor Unveils Changes in Novel Molecular Mechanism Driving Neuroprotection in Alzheimer's Disease in <i>in vitro</i> and <i>in vivo</i> Models Open
View article: Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors Open
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 …
View article: 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
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 Open
With innumerable clinical failures of target-specific drug candidates for multifactorial diseases, such as Alzheimer's disease (AD), which remains inefficiently treated, the advent of multitarget drug discovery has brought a new breath of …
View article: 2-(Piperidin-4-yl)acetamides as Potent Inhibitors of Soluble Epoxide Hydrolase with Anti-Inflammatory Activity
2-(Piperidin-4-yl)acetamides as Potent Inhibitors of Soluble Epoxide Hydrolase with Anti-Inflammatory Activity Open
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 pot…
View article: From the Design to the <i>In Vivo</i> Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis
From the Design to the <i>In Vivo</i> Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis Open
The pharmacological inhibition of soluble epoxide hydrolase (sEH) is efficient for the treatment of inflammatory and pain-related diseases. Numerous potent sEH inhibitors (sEHIs) present adamantyl or phenyl moieties, such as the clinical c…
View article: Inhibition of Soluble Epoxide Hydrolase Ameliorates Phenotype and Cognitive Abilities in a Murine Model of Niemann Pick Type C Disease
Inhibition of Soluble Epoxide Hydrolase Ameliorates Phenotype and Cognitive Abilities in a Murine Model of Niemann Pick Type C Disease Open
Niemann–Pick type C (NPC) disease is a rare autosomal recessive inherited childhood neurodegenerative disease characterized by the accumulation of cholesterol and glycosphingolipids, involving the autophagy-lysosome system. Inhibition of s…
View article: Soluble Epoxide Hydrolase Inhibition Ameliorates Phenotype and Cognitive Capabilities in a Murine Model of Niemann Pick Disease Type C
Soluble Epoxide Hydrolase Inhibition Ameliorates Phenotype and Cognitive Capabilities in a Murine Model of Niemann Pick Disease Type C Open
Niemann-Pick type C (NPC) disease is a childhood autosomal recessive inherited rare neuro-degenerative disease, characterized by the accumulation of cholesterol and glycosphingolipids, implicating the autophagy-lysosome system. Inhibition …
View article: 2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: <i>In Vivo</i> Evaluation in a Murine Model of Acute Pancreatitis
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: <i>In Vivo</i> Evaluation in a Murine Model of Acute Pancreatitis Open
In vivo pharmacological inhibition of soluble epoxide hydrolase (sEH) reduces inflammatory diseases, including acute pancreatitis (AP). Adamantyl ureas are very potent sEH inhibitors, but the lipophilicity and metabolism of the adam…
View article: Pharmacological Inhibition of Soluble Epoxide Hydrolase as a New Therapy for Alzheimer's Disease
Pharmacological Inhibition of Soluble Epoxide Hydrolase as a New Therapy for Alzheimer's Disease Open
View article: Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors Open
View article: Pharmacological inhibition of soluble epoxide hydrolase as a new therapy for Alzheimer’s Disease
Pharmacological inhibition of soluble epoxide hydrolase as a new therapy for Alzheimer’s Disease Open
The inhibition of the enzyme soluble epoxide hydrolase (sEH) has demonstrated clinical therapeutic effects in several peripheral inflammatory-related diseases, with two compounds that have entered clinical trials. However, the role of this…
View article: CCDC 1554197: Experimental Crystal Structure Determination
CCDC 1554197: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1554198: Experimental Crystal Structure Determination
CCDC 1554198: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Aniline-Based Inhibitors of Influenza H1N1 Virus Acting on Hemagglutinin-Mediated Fusion
Aniline-Based Inhibitors of Influenza H1N1 Virus Acting on Hemagglutinin-Mediated Fusion Open
Two series of easily accessible anilines were identified as inhibitors of influenza A virus subtype H1N1, and extensive chemical synthesis and analysis of the structure-activity relationship were performed. The compounds were shown to inte…