Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors

Ashraf Brik, John Muldoon, Ying Chuan Lin, John H. Elder, David S. Goodsell, Arthur J. Olson, Valery V. Fokin, K. Bary Sharpless, Chi Huey Wong

Research output: Contribution to journalArticle

139 Citations (Scopus)

Abstract

Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.

Original languageEnglish
Pages (from-to)1246-1248
Number of pages3
JournalChemBioChem
Volume4
Issue number11
DOIs
Publication statusPublished - 7 Nov 2003
Externally publishedYes

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Keywords

  • Click chemistry
  • Enzyme
  • HIV protease
  • Inhibitors
  • Screening

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Biochemistry, Genetics and Molecular Biology(all)

Cite this

Brik, A., Muldoon, J., Lin, Y. C., Elder, J. H., Goodsell, D. S., Olson, A. J., ... Wong, C. H. (2003). Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors. ChemBioChem, 4(11), 1246-1248. https://doi.org/10.1002/cbic.200300724