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Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities

Faist, J. and Seebacher, W. and Kaiser, M. and Brun, R. and Saf, R. and Weis, R.. (2010) Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities. European Journal of Medicinal Chemistry, 45 (1). pp. 179-185.

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Official URL: http://edoc.unibas.ch/dok/A5843075

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Abstract

N-Alkyl and N-(2-dialkylaminoethyl) derivatives of 5-amino-2-azabicyclo-nonanes were prepared and tested in vitro for their activities against the multidrug-resistant K1 strain of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). Most of the new compounds showed lower antitrypanosomal activity than their parent compounds. With respect to their activity against P. falciparum the N-alkyl derivatives exhibited worse selectivity due to decreased antiplasmodial activity or higher cytotoxicity. In comparison all of the new N-(2-dialkylaminoethyl) analogues possessed a much better selectivity and a single of these compounds showed even better antiplasmodial activity and selectivity than chloroquine
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:EDIFOR
ISSN:0223-5234
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:05 Dec 2017 09:59
Deposited On:08 Jun 2012 06:47

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