| Synthesis and evaluation of the antitrypanosomal and antiplasmodial activities of new 4-aminobicyclo[2.2.2]octane derivatives. | |
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MedLine Citation:
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PMID: 15913846 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Werner Seebacher; Reto Brun; Marcel Kaiser; Robert Saf; Robert Weis |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: 40 ISSN: 0223-5234 ISO Abbreviation: Eur J Med Chem Publication Date: 2005 Sep |
Date Detail:
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Created Date: 2005-09-30 Completed Date: 2006-01-24 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: France |
Other Details:
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Languages: eng Pagination: 888-96 Citation Subset: IM |
Affiliation:
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Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitätsplatz 1, A-8010 Graz, Austria. we.seebacher@uni-graz.at |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals 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* Rats Trypanocidal Agents / chemical synthesis*, chemistry, pharmacology* Trypanosoma brucei rhodesiense / drug effects* |
| Chemical | |
Reg. No./Substance:
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0/4-aminobicyclo(2.2.2)octane; 0/Antimalarials; 0/Bicyclo Compounds; 0/Trypanocidal Agents |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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