QSAR guided synthesis of simplified antiplasmodial analogs of naphthylisoquinoline alkaloids

Bringmann, G. and Bischof, S. K. and Müller, S. and Gulder, T. and Winter, C. and Stich, A. and Moll, H. and Kaiser, M. and Brun, R. and Dreher, J. and Baumann, K.. (2010) QSAR guided synthesis of simplified antiplasmodial analogs of naphthylisoquinoline alkaloids. European journal of medicinal chemistry, 45 (11). pp. 5370-5383.

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Official URL: http://edoc.unibas.ch/dok/A5843000

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Naphthylisoquinoline alkaloids have attracted considerable interest because of their intriguing structure, their unique biosynthetic origin, and their biological activities against several pathogens causing tropical diseases. Their promising pharmacologic properties make them suitable lead structures for new agents, in particular against malaria. Since these natural products are not easy to isolate in sufficient quantities or to synthesize stereoselectively, quantitative structure-activity relationship studies were accomplished to find new antiplasmodial analogs that are structurally related to the naturally occurring naphthylisoquinoline alkaloids, but more easily accessible, more active against Plasmodium falciparum, and, last but not least, less toxic. We report on the synthesis of several simplified compounds by a Suzuki coupling between the naphthalene and the isoquinoline moieties and on their activities against different pathogens causing infectious diseases. Some structures were found to exhibit excellent--and selective--activities against P. falciparum in vitro
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
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:05 Dec 2017 10:02
Deposited On:14 Sep 2012 06:46

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