2. Academic Validation
  3. Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates

Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates

  • Eur J Med Chem. 2009 Feb;44(2):736-44. doi: 10.1016/j.ejmech.2008.05.002.
Christian Schlapper 1,  Werner Seebacher,  Johanna Faist,  Marcel Kaiser,  Reto Brun,  Robert Saf,  Robert Weis
Affiliations

Affiliation

  • 1 Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitätsplatz 1, A-8010 Graz, Austria.
PMID: 18571774 DOI: 10.1016/j.ejmech.2008.05.002
Abstract

Several 4-aminobicyclo[2.2.2]octyl esters of omega-dialkylamino acids were prepared. Their activities against the multidrug-resistant K(1) strain of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900) were determined using microplate assays and compared to those of formerly prepared analogues. The biological activity was influenced by the relative configuration in ring position 2, by the chain length of the acid moiety and by the amino substitution. The most active antiplasmodial ester was as active as chloroquine. One of the new compounds exhibited the highest antitrypanosomal activity and selectivity of all bicyclo-octane derivatives prepared so far.

Figures