Document Detail

Synthesis and evaluation of the antitrypanosomal and antiplasmodial activities of new 4-aminobicyclo[2.2.2]octane derivatives.
MedLine Citation:
PMID:  15913846     Owner:  NLM     Status:  MEDLINE    
Several new 4-amino-6,7-diphenylbicyclo[2.2.2]octane derivatives, methylthiosemicarbazones of bicyclo[2.2.2]octan-2-ones and esters of bicyclo[2.2.2]octan-2-ols were prepared. Their antitrypanosomal activities against Trypanosoma brucei rhodesiense (STIB 900) and their antiplasmodial activity against the K1 strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) were investigated using microplate assays. In addition to that, the cytotoxicity of the new compounds was determined using L-6 cells. The methylthiosemicarbazones show moderate antiprotozoal activities whereas some of the esters of piperonylic acid, homopiperonylic acid and 2-naphtoic acid exhibit remarkable antitrypanosomal and antiplasmodial activity.
Werner Seebacher; Reto Brun; Marcel Kaiser; Robert Saf; Robert Weis
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  40     ISSN:  0223-5234     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2005 Sep 
Date Detail:
Created Date:  2005-09-30     Completed Date:  2006-01-24     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  888-96     Citation Subset:  IM    
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitätsplatz 1, A-8010 Graz, Austria.
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MeSH Terms
Antimalarials / chemical synthesis*,  chemistry,  pharmacology*
Bicyclo Compounds / chemistry*
Cell Line
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Molecular Structure
Myoblasts, Skeletal / drug effects
Parasitic Sensitivity Tests
Plasmodium falciparum / drug effects*
Trypanocidal Agents / chemical synthesis*,  chemistry,  pharmacology*
Trypanosoma brucei rhodesiense / drug effects*
Reg. No./Substance:
0/4-aminobicyclo(2.2.2)octane; 0/Antimalarials; 0/Bicyclo Compounds; 0/Trypanocidal Agents

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