Antimalarial sulfone trioxanes

Gary H. Posner, Hardwin O'Dowd, Thomas Caferro, Jared N. Cumming, Poonsakdi Ploypradith, Suji Xie, Theresa A. Shapiro

Research output: Contribution to journalArticlepeer-review

Abstract

A series of new sulfide and sulfone 1,2,4-trioxanes was prepared in only a few steps from commercial reactants. The sulfone trioxanes were found to have higher in vitro antimalarial potencies than the sulfides, with 12β- arylsulfone trioxanes 1β being from 1/3 to 1/4 as potent as the complex natural antimalarial trioxane artemisinin (2). A tentative chemical mechanism is proposed to account for the great difference in antimalarial activity of the 12α- vs. 12β-sulfide trioxanes.

Original languageEnglish (US)
Pages (from-to)2273-2276
Number of pages4
JournalTetrahedron Letters
Volume39
Issue number16
DOIs
StatePublished - Apr 16 1998

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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