4-Aminobicyclo[2.2.2]octanone Derivatives with Antiplasmodial and Antitrypanosomal Activities |
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| Authors: | Werner?Seebacher Reto?Brun Robert?Saf Email author" target="_blank">Robert?WeisEmail author |
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| Institution: | (1) Institute of Pharmaceutical Chemistry and Pharmaceutical Technology, University of Graz, A-8010 Graz, Austria, AT;(2) Swiss Tropical Institute, Basel, Switzerland, CH;(3) Institute of Chemical Technology of Organic Materials, University of Technology, Graz, Austria, AT |
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| Abstract: | Summary. 4-Aminobicyclo2.2.2]octanones were converted to their N-oxides and to 4-aminobicyclo2.2.2]octanes. Furthermore, the 6,7-bis-(4-methoxyphenyl) analogues were synthesized. All products were screened for their activities against Trypanosoma b. rhodesiense and Plasmodium falciparum. The pharmacological results were compared with those of formerly tested bicyclo2.2.2]octanones and bicyclo2.2.2]octanols. Structure-activity relationships are discussed.Received April 8, 2003; accepted April 14, 2003
Published online September 25, 2003 |
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| Keywords: | , Antiplasmodial activity, Antitrypanosomal activity, Bicyclo[2,2,2]octane derivatives, Reductions, Oxidations, |
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