Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 2, Pages 565-570Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.020
Keywords
sEH inhibitor; Anti-GBM glomerulonephritis rat model; Spirocyclic diamine; Urea; Chronic kidney diseases
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Funding
- Grants-in-Aid for Scientific Research [23102014, 23310148] Funding Source: KAKEN
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We identified 1-oxa-4,9-diazaspiro[5.5]undecane-based trisubstituted ureas as highly potent soluble epoxide hydrolase (sEH) inhibitors and orally active agents for treating chronic kidney diseases. Compound 19 exhibited excellent sEH inhibitory activity and bioavailability. When administered orally at 30 mg/kg, 19 lowered serum creatinine in a rat model of anti-glomerular basement membrane glomerulonephritis but 2,8-diazaspiro[4.5]decane-based trisubstituted ureas did not. These results suggest that 19 is an orally active drug candidate for treating chronic kidney diseases. (C) 2013 Elsevier Ltd. All rights reserved.
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