Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: heterocyclic bioisosteres for the urea group in DuP 128

Richard G. Wilde, John D. Klaczkiewicz, Jeffrey T. Billheimer, Ruth R. Wexler, Peter J. Gillies

Research output: Contribution to journalArticle

9 Scopus citations

Abstract

A series of compounds bearing two heterocyclic substituents were evaluated for inhibition of the ACAT enzyme. One heterocyclic group was chosen to mimic the urea group in our clinical candidate, DuP 128. Of the several groups examined, aminobenzoxazoles proved to be the most potent in terms of inhibition of ACAT in J774 macrophage cells.

Original languageEnglish (US)
Pages (from-to)177-180
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number2
DOIs
StatePublished - Jan 19 1995
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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