Antiprotozoal Activities of Epimeric Aminobicycles |
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| Authors: | Werner Seebacher Marcel Kaiser Reto Brun Robert Saf Robert Weis |
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| Institution: | (1) Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University of Graz, Graz, Austria;(2) Swiss Tropical Institute, Basel, Switzerland;(3) Institute of Chemical Technology of Organic Materials, Erzherzog-Johann University, Graz, Austria |
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| Abstract: | Summary. We synthesized several 4-aminobicyclo2.2.2] octan-2-ols and 4-amino-2-azabicyclo3.2.2]nonanes from epimerized 4-amino-bicyclo2.2.2]octan-2-ones.
The new compounds were tested for their activity against Trypanosoma b. rhodesiense, the causative organism of East African sleeping sickness, and Plasmodium falciparum K
1, a multiresistant protozoan parasite which causes Malaria tropica. The results are compared to the activities of their formerly
synthesized stereoisomers and structure–activity relationships are discussed. |
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| Keywords: | , East African sleeping sickness, Malaria tropica, Bicyclic compounds, Configuration, Structure–,activity relationships, |
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