Antimalarially potent, easily prepared, fluorinated endoperoxides

Gary H. Posner, Xueliang Tao, Jared N. Cumming, Donna Klinedinst, Theresa A. Shapiro

Research output: Contribution to journalArticlepeer-review

Abstract

Three or four step chemical synthesis and in vitro antimalarial testing showed crystalline, thermally stable, bicyclic endoperoxides 3c and 4c to be potent antimalarials, having approximately 15% of the antimalarial activity of the clinically used, complex, sesquiterpene, lactone, natural product artemisinin (qinghaosu, 1). A novel mechanism involving reactive alkylating agents is proposed to account for the ability of endoperoxides 3c and 4c to kill malaria parasites.

Original languageEnglish (US)
Pages (from-to)7225-7228
Number of pages4
JournalTetrahedron Letters
Volume37
Issue number40
DOIs
StatePublished - Sep 30 1996

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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