2. Academic Validation
  3. Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals

Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals

  • Bioorg Med Chem. 2007 Aug 15;15(16):5543-50. doi: 10.1016/j.bmc.2007.05.042.
Christian Schlapper 1,  Werner Seebacher,  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: 17544672 DOI: 10.1016/j.bmc.2007.05.042
Abstract

A couple of bicyclo[2.2.2]octyl esters of 2-dialkylaminoacetic acids were prepared. Their antiplasmodial and antitrypanosomal activities against Trypanosoma brucei rhodesiense (STIB 900) and the K(1) strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) were determined using microplate assays. Structure-activity relationships were discussed. The antiprotozoal activities were remarkably increased by insertion of a second basic centre. The selectivity indices of the most active compounds are superior in the bicyclo-octane series.

Figures