Design and synthesis of endoperoxide antimalarial prodrug models

Paul M. O'Neill, Paul A. Stocks, Matthew D. Pugh, Nuna C. Araujo, Edward E. Korshin, Jamie F. Bickley, Stephen A. Ward, Patrick G. Bray, Erica Pasini, Jill Davies, Edite Verissimo, Mario D. Bachi

Research output: Contribution to journalArticlepeer-review

61 Scopus citations


A masked combination chemotherapy which relies on the embedding of a number of active components, in a latent form, within a single endoperoxidic chemical entity is the aim of the research presented. The approach is illustrated by means of purposely designed bicyclic endoperoxide prodrug prototypes 1 and subsequently validated through the study of model compounds 2 (Ar= Ph, p-FC 6H4, p-ClC6H4.

Original languageEnglish
Pages (from-to)4193-4197
Number of pages5
JournalAngewandte Chemie - International Edition
Issue number32
StatePublished - 13 Aug 2004
Externally publishedYes


  • Antimalarial agents
  • Chalcones
  • Combination chemotherapy
  • Cysteine protease inhibitors
  • Endoperoxides


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