Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives

Alexander Khrizman, Rachel D. Slack, Richard C. Remsing, Susan Little, Vanessa Yardley, Guillermo Moyna

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.

Original languageEnglish (US)
Pages (from-to)569-576
Number of pages8
JournalArchiv der Pharmazie
Volume340
Issue number11
DOIs
StatePublished - Nov 2007
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Drug Discovery

Keywords

  • Hydrazynes
  • Parasitoses
  • Protozoocidal activity
  • Synthesis
  • Tropolone derivatives

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