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

Johanna Faist; Werner Seebacher; Christian Schlapper; Marcel Kaiser; Reto Brun; Robert Saf; Robert Weis

doi:10.1016/j.bmc.2009.04.002

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. Epub 2009 Apr 7.

Authors

Johanna Faist¹, Werner Seebacher, Christian Schlapper, Marcel Kaiser, Reto Brun, Robert Saf, Robert Weis

Affiliation

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.

MeSH terms

Amides / chemical synthesis
Amides / chemistry*
Amino Acids / chemistry*
Animals
Antimalarials / chemical synthesis
Antimalarials / chemistry
Antimalarials / toxicity*
Bridged Bicyclo Compounds / chemical synthesis
Bridged Bicyclo Compounds / chemistry
Bridged Bicyclo Compounds / toxicity*
Esters / chemical synthesis
Esters / chemistry
Parasitic Sensitivity Tests
Plasmodium berghei / drug effects
Plasmodium falciparum / drug effects
Structure-Activity Relationship
Trypanocidal Agents / chemical synthesis
Trypanocidal Agents / chemistry
Trypanocidal Agents / toxicity*
Trypanosoma brucei rhodesiense / drug effects

Substances

Amides
Amino Acids
Antimalarials
Bridged Bicyclo Compounds
Esters
Trypanocidal Agents