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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 journal › Article › peer-review

165 Scopus citations

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
StatePublished - 7 Nov 2003
Externally publishedYes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry

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