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The antiplasmodial and antitrypanosomal activities of novel piperazine derivatives of 3-azabicyclo[3.2.2]nonanes

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Abstract

Some new piperazine derivatives of antiprotozoal active 3-azabicyclo[3.2.2]nonanes were prepared. Verification of the structures of the new compounds was done by one- and two-dimensional NMR measurements. All new compounds were investigated for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum NF54 and Trypanosoma brucei rhodesiense. Their cytotoxicity was assessed against L6 cells. Some of the new compounds showed in vitro very good antiplasmodial and excellent antitrypanosomal activities. The most antitrypanosomal active compound was screened in vivo in a mouse model against T. b. rhodesiense.

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Authors and Affiliations

  1. Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan

    Noor-Ul-Amin Mohsin

  2. Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria

    Werner Seebacher, Johanna Faist, Patrick Hochegger & Robert Weis

  3. Swiss Tropical and Public Health Institute and University of Basel, Basel, Switzerland

    Marcel Kaiser & Pascal Mäser

  4. Institute for Chemistry and Technology of Materials (ICTM), Graz University of Technology, Graz, Austria

    Robert Saf

Authors
  1. Noor-Ul-Amin Mohsin
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  2. Werner Seebacher
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  3. Johanna Faist
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  4. Patrick Hochegger
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  5. Marcel Kaiser
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  6. Pascal Mäser
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  7. Robert Saf
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  8. Robert Weis
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Corresponding author

Correspondence to Werner Seebacher.

Ethics declarations

In vivo efficacy studies in mice were conducted at the Swiss Tropical and Public Health Institute (Basel) according to the rules and regulations for the protection of animal rights (“Tierschutzverordnung”) of the Swiss “Bundesamt für Veterinärwesen”. They were approved by the veterinary office of Canton Basel-Stadt, Switzerland.

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Mohsin, NUA., Seebacher, W., Faist, J. et al. The antiplasmodial and antitrypanosomal activities of novel piperazine derivatives of 3-azabicyclo[3.2.2]nonanes. Monatsh Chem 149, 99–109 (2018). https://doi.org/10.1007/s00706-017-2109-3

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  • DOI: https://doi.org/10.1007/s00706-017-2109-3

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