Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
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.
Faist
Johanna
J
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria.
Seebacher
Werner
W
Schlapper
Christian
C
Kaiser
Marcel
M
Brun
Reto
R
Saf
Robert
R
Weis
Robert
R
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry*; D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects
D000577:Amides; D000596:Amino Acids; D000962:Antimalarials; D001643:Bridged Bicyclo Compounds; D004952:Esters; D014344:Trypanocidal Agents