Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing heterocyclic groups bioisosteric for an imidazole

Richard G. Wilde, Jeffrey T. Billheimer, Sandra J. Germain, Peter J. Gillies, C. Anne Higley, Hollis S. Kezar, Thomas P. Maduskuie, Edward S. Shimshick, Ruth R. Wexler

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

Abstract

A series of compounds bearing heterocyclic substituents were prepared, and evaluated for inhibition of the ACAT enzyme. The heterocyclic groups were compared in terms of in vitro potency against their diarylimidazole analogues. Data for the purposes of QSAR were also collected. Our goal is a systemic ACAT inhibitor, which would be a potential antihypercholesterolemic and antiatherosclerotic agent.

Original languageEnglish (US)
Pages (from-to)167-172
Number of pages6
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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