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

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

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)5773-5777
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number22
DOIs
StatePublished - 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

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