Syntheses of FDA approved HIV protease inhibitors

A. K. Ghosh*, G. Bilcer, G. Schiltz

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

152 Scopus citations


The treatment of HIV and AIDS was revolutionized by the introduction of peptidomimetic aspartyl protease inhibitors. One of the major limitations of this type of therapy is that higher therapeutic doses are necessary because of the presence of 'peptide-like' features in the drugs. Therefore, adequate supplies and cost effective syntheses of these drugs are of utmost importance. To date, there are six protease inhibitors approved by the United States Food and Drug Administration (FDA) for the treatment of HIV and AIDS. This review focuses on the published syntheses of currently FDA approved HIV protease inhibitor drugs, their isosteres and ligands.

Original languageEnglish (US)
Pages (from-to)2203-2229
Number of pages27
Issue number15
StatePublished - 2001


  • HIV
  • Inhibitor
  • Isostere
  • Protease
  • Synthesis

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry


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