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Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids
Authors:Johanna Faist  Werner Seebacher  Christian Schlapper  Marcel Kaiser  Reto Brun  Robert Saf  Robert Weis
Institution:1. Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria;2. Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland;3. Institute of Chemical Technology of Organic Materials, Erzherzog-Johann University, Stremayrgasse 26/1, A-8010 Graz, Austria
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.
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