Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead

Johanna Faist, Werner Seebacher, Robert Saf, Reto Brun, Marcel Kaiser, Robert Weis

Research output: Contribution to journalArticlepeer-review

Abstract

Several dimethylamino-derivatives of the new compound-class 3-azabicyclo[3.2.2]nonanes were prepared. For better comparison of activity also a few analogues of bicyclo[2.2.2]octanes and 2-azabicyclo[3.2.2]nonanes were synthesized. Their activities were examined in vitro against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). A couple of the newly synthesized compounds showed promising antiprotozoal activity and selectivity. The results of the biological tests of the novel compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure–activity relationships were discussed.
Original languageEnglish
Pages (from-to)3781-3789
JournalBioorganic & Medicinal Chemistry
Volume24
Issue number16
DOIs
Publication statusPublished - 2016

Treatment code (Nähere Zuordnung)

  • Basic - Fundamental (Grundlagenforschung)

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  • Mass Spectrometry

    Saf, R. & Bartl, K.

    1/01/95 → …

    Project: Research area

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