Design and Potency of Dual Soluble Epoxide Hydrolase/Fatty Acid Amide Hydrolase Inhibitors
نویسندگان
چکیده
منابع مشابه
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.
Multi-target inhibitors have become increasing popular as a means to leverage the advantages of poly-pharmacology while simplifying drug delivery. Here, we describe dual inhibitors for soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FAAH), two targets known to synergize when treating inflammatory and neuropathic pain. The structure activity relationship (SAR) study described her...
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Inhibitors of soluble epoxide hydrolase (sEH) represent one of the novel pharmaceutical approaches for treating hypertension, vascular inflammation, pain and other cardiovascular related diseases. Most of the potent sEH inhibitors reported in literature often suffer from poor solubility and bioavailability. Toward improving pharmacokinetic profile beside favorable potency, two series of 4-benza...
متن کاملDesign, Synthesis and Biological Evaluation of 4-Benzamidobenzoic Acid Hydrazide Derivatives as Novel Soluble Epoxide Hydrolase Inhibitors
Inhibitors of soluble epoxide hydrolase (sEH) represent one of the novel pharmaceutical approaches for treating hypertension, vascular inflammation, pain and other cardiovascular related diseases. Most of the potent sEH inhibitors reported in literature often suffer from poor solubility and bioavailability. Toward improving pharmacokinetic profile beside favorable potency, two series of 4-benza...
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A series of novel Dual Inhibitors of COX-2 and sEH containing an N-urea substituted pyrazole as a lead for sEH inhibition have been synthesized and screened as novel analogues to reduce blood pressure elevation by acting as sEH inhibitors. The synthesized compounds having varying degrees of selectivity towards the sEH enzymes. Particularly compounds 6g and 6i emerged as the most potent sEH inhi...
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Soluble epoxide hydrolase enzyme is a promising therapeutic target for hypertension, vascular inflammation, pain and some other risk factors of cardiovascular diseases. The most potent sEH inhibitors reported in the literature are urea-based ones which often have poor bioavailability. In this study, in a quest for finding potent inhibitors of soluble epoxide hydrolase, some 4,6-disubstituted py...
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ژورنال
عنوان ژورنال: ACS Omega
سال: 2018
ISSN: 2470-1343,2470-1343
DOI: 10.1021/acsomega.8b01625