Abstract
A 192-member library of N,N′-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or para/meta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ionizable groups close to the urea group dramatically decreased their activities.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 5773-5777 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 16 |
| Issue number | 22 |
| DOIs | |
| State | Published - Nov 15 2006 |
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Keywords
- Anti-inflammation
- Hypertension
- Soluble epoxide hydrolase
- Urea
ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors. / Hwang, Sung Hee; Morisseau, Christophe; Do, Zung; Hammock, Bruce D.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 22, 15.11.2006, p. 5773-5777.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors
AU - Hwang, Sung Hee
AU - Morisseau, Christophe
AU - Do, Zung
AU - Hammock, Bruce D.
PY - 2006/11/15
Y1 - 2006/11/15
N2 - A 192-member library of N,N′-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or para/meta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ionizable groups close to the urea group dramatically decreased their activities.
AB - A 192-member library of N,N′-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or para/meta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ionizable groups close to the urea group dramatically decreased their activities.
KW - Anti-inflammation
KW - Hypertension
KW - Soluble epoxide hydrolase
KW - Urea
UR - http://www.scopus.com/inward/record.url?scp=33749251458&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33749251458&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2006.08.078
DO - 10.1016/j.bmcl.2006.08.078
M3 - Article
C2 - 16949285
AN - SCOPUS:33749251458
VL - 16
SP - 5773
EP - 5777
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 22
ER -