Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors

Sung Hee Hwang; Christophe Morisseau; Zung Do; Bruce D. Hammock

doi:10.1016/j.bmcl.2006.08.078

Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors

Sung Hee Hwang, Christophe Morisseau, Zung Do, Bruce D. Hammock

Entomology

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26 Scopus citations

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	https://doi.org/10.1016/j.bmcl.2006.08.078
State	Published - Nov 15 2006

Keywords

Anti-inflammation
Hypertension
Soluble epoxide hydrolase
Urea

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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10.1016/j.bmcl.2006.08.078

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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.",

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AU - Hwang, Sung Hee

AU - Morisseau, Christophe

AU - Do, Zung

AU - Hammock, Bruce D.

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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.

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KW - Hypertension

KW - Soluble epoxide hydrolase

KW - Urea

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Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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