Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates

Fu Sen Liang, Ashraf Brik, Ying Chuan Lin, John H. Elder, Chi Huey Wong

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

A method utilizing the strategy of epoxide opening by amine with water as co-solvent and screening in situ was developed for rapid discovery of protein inhibitors. Using this approach, HIV protease inhibitors with novel P1′ residues were identified in our study. This strategy should be applicable for the efficient assembly of diverse compound collections for inhibitors' discovery and optimization in other systems.

Original languageEnglish
Pages (from-to)1058-1062
Number of pages5
JournalBioorganic and Medicinal Chemistry
Volume14
Issue number4
DOIs
StatePublished - 15 Feb 2006
Externally publishedYes

Keywords

  • Epoxide opening
  • HIV protease inhibitors
  • In situ screening
  • In water

ASJC Scopus subject areas

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

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