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Spiroindolones, a potent compound class for the treatment of malaria

Rottmann, M. and McNamara, C. and Yeung, B. K. and Lee, M. C. and Zou, B. and Russell, B. and Seitz, P. and Plouffe, D. M. and Dharia, N. V. and Tan, J. and Cohen, S. B. and Spencer, K. R. and Gonzalez-Paez G. E., and Lakshminarayana, S. B. and Goh, A. and Suwanarusk, R. and Jegla, T. and Schmitt, E. K. and Beck, H. P. and Brun, R. and Nosten, F. and Renia, L. and Dartois, V. and Keller, T. H. and Fidock, D. A. and Winzeler, E. A. and Diagana, T. T.. (2010) Spiroindolones, a potent compound class for the treatment of malaria. Science, Vol. 329, no. 5996. pp. 1175-1180.

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Official URL: http://edoc.unibas.ch/dok/A5843025

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Abstract

Recent reports of increased tolerance to artemisinin derivatives--the most recently adopted class of antimalarials--have prompted a need for new treatments. The spirotetrahydro-beta-carbolines, or spiroindolones, are potent drugs that kill the blood stages of Plasmodium falciparum and Plasmodium vivax clinical isolates at low nanomolar concentration. Spiroindolones rapidly inhibit protein synthesis in P. falciparum, an effect that is ablated in parasites bearing nonsynonymous mutations in the gene encoding the P-type cation-transporter ATPase4 (PfATP4). The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model
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 Beck, Hans-Peter
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:American Association for the Advancement of Science
ISSN:0036-8075
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:08 Jun 2012 06:56
Deposited On:08 Jun 2012 06:47

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