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Synthesis and antimalarial activity of some neocryptolepine analogues carrying a multifunctional linear and branched carbon-side chains

Shaban, E. and Wicht, K. J. and Wang, N. and Mei, Z. W. and Hayashi, I. and El Gokha, A. A. A. and Kaiser, M. and El Sayed, I. E. and Egan, T. J. and Inokuchi, T.. (2015) Synthesis and antimalarial activity of some neocryptolepine analogues carrying a multifunctional linear and branched carbon-side chains. Heterocycles, Vol. 89, H. 4. pp. 1055-1064.

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Official URL: http://edoc.unibas.ch/dok/A6348545

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Abstract

The synthesis and in vitro antimalarial activity of several neocryptolepine analogues carrying either a linear or branched dibasic side chain at C11 are described. Many of these neocryptolepine analogues have low nanomolar antimalarial activity against the chloroquine-sensitive P. falciparum strain (NF54). The data also dernonstrated that a branched structural motif is not superior for antimalarial activity over a linear side chain, but their thioureido derivatives showed lower cytotoxicity than the linear one. Ureido and thioureido derivatives also showed stronger beta-haematin inhibition than the corresponding free amines
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 > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Elsevier
ISSN:0385-5414
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:10 Apr 2015 09:12
Deposited On:10 Apr 2015 09:12

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