Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids

  • Bioorg Med Chem. 2009 May 15;17(10):3595-603. doi: 10.1016/j.bmc.2009.04.002.
Johanna Faist  1 ,  Werner Seebacher ,  Christian Schlapper ,  Marcel Kaiser ,  Reto Brun ,  Robert Saf ,  Robert Weis
Affiliations
  • 1. Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria.
PMID: 19395265 DOI: 10.1016/j.bmc.2009.04.002
Abstract

Several bicyclic amides and esters of dialkylamino acids were prepared. Their activities against a multiresistant strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900) were examined. Structure-activity relationships were discussed. Particularly the ester compounds showed good antiplasmodial and antitrypanosomal activity and a single compound was tested in vivo against Plasmodium berghei.