Inhibitors of HIV-1 protease by using in situ click chemistry

Matthew Whiting, John Muldoon, Ying Chuan Lin, Steven M. Silverman, William Lindstrom, Arthur J. Olson, Hartmuth C. Kolb, M. G. Finn, K. Barry Sharpless, John H. Elder, Valery V. Fokin

Research output: Contribution to journalArticle

421 Citations (Scopus)

Abstract

(Chemical Equation Presented) Twice poor equals potent: HIV-1 Protease assembles its own potent inhibitor through formation of the triazole linkage from azide- and alkyne-containing fragments that are themselves poor binders.

Original languageEnglish
Pages (from-to)1435-1439
Number of pages5
JournalAngewandte Chemie - International Edition
Volume45
Issue number9
DOIs
Publication statusPublished - 20 Feb 2006
Externally publishedYes

Keywords

  • Click chemistry
  • Drug design
  • HIV-1 protease
  • Inhibitors
  • Triazoles

ASJC Scopus subject areas

  • Chemistry(all)

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  • Cite this

    Whiting, M., Muldoon, J., Lin, Y. C., Silverman, S. M., Lindstrom, W., Olson, A. J., Kolb, H. C., Finn, M. G., Sharpless, K. B., Elder, J. H., & Fokin, V. V. (2006). Inhibitors of HIV-1 protease by using in situ click chemistry. Angewandte Chemie - International Edition, 45(9), 1435-1439. https://doi.org/10.1002/anie.200502161