Abstract:
:A series of inhibitors of the soluble epoxide hydrolase (sEH) containing two urea groups has been developed. Inhibition potency of the described compounds ranges from 2.0 μM to 0.4 nM. 1,6-(Hexamethylene)bis[(adamant-1-yl)urea] (3b) was found to be a potent slow tight binding inhibitor (IC50=0.5 nM) with a strong binding to sEH (Ki=3.1 nM) and a moderately long residence time on the enzyme (koff=1.05 × 10(-3) s(-1); t1/2=11 min).
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Burmistrov V,Morisseau C,Lee KS,Shihadih DS,Harris TR,Butov GM,Hammock BDdoi
10.1016/j.bmcl.2014.03.016subject
Has Abstractpub_date
2014-05-01 00:00:00pages
2193-7issue
9eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)00232-7journal_volume
24pub_type
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