title: Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity.
abstract: Dialkylaminoalkyl derivatives of 2-azabicyclo[3.2.2]nonanes and of bicyclo[2.2.2]octanes were prepared and their activities determined in vitro against the multiresistant K1 strain of Plasmodium falciparum. Several of the new compounds exhibited very promising antiplasmodial activity and selectivity. The results were compared to those of formerly synthesized analogues and of drugs in use. Structure-activity relationships were detected. Some of the more potent compounds were tested in vivo against Plasmodium berghei showing weak to moderate activity. A single compound was able to increase the mean survival days of infected mice.
authors: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria.
authors: Johanna
authors: J
authors: Faist
authors: Werner
authors: W
authors: Seebacher
authors: Marcel
authors: M
authors: Kaiser
authors: Reto
authors: R
authors: Brun
authors: Robert
authors: R
authors: Saf
authors: Robert
authors: R
authors: Weis
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D053961:Azabicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D004195:Disease Models, Animal; D051379:Mice; D032448:Myoblasts, Skeletal / Q000187:drug effects; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D053961:Azabicyclo Compounds; D001643:Bridged Bicyclo Compounds