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Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities

Seebacher, Werner and Wolkinger, Volker and Faist, Johanna and Kaiser, Marcel and Brun, Reto and Saf, Robert and Bucar, Franz and Gröblacher, Barbara and Brantner, Adelheid and Merino, Virginia and Kalia, Yogeshvar and Scapozza, Leonardo and Perozzo, Remo and Weis, Robert. (2015) Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities. Bioorganic & medicinal chemistry letters, Vol. 25, H. 7. pp. 1390-1393.

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Official URL: http://edoc.unibas.ch/dok/A6373548

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Abstract

Several bicyclic compounds, 3-azabicyclo[3.2.2]nonanes, have been prepared. The new compounds were tested for their activities against one strain of the causative organism of Malaria tropica, Plasmodium falciparum K1, which is resistant against chloroquine and pyrimethamine. In addition, their cytotoxicity and their activity against the pathogen of the East African form of sleeping sickness, Trypanosoma brucei rhodesiense, were investigated. Structure-activity relationships are discussed considering data of readily prepared compounds. For the first time, a distinct in vivo activity was observed against Plasmodium berghei in a mouse model. The active compound was further investigated.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel and Brun, Reto
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0960-894X
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:05 Jun 2015 08:53
Deposited On:05 Jun 2015 08:53

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