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Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with anti-parasitic activity

Holloway, G. A. and Charman, W. N. and Fairlamb, A. H. and Brun, R. and Kaiser, M. and Kostewicz, E. and Novello, P. M. and Parisot, J. P. and Richardson, J. and Street, I. P. and Watson, K. G. and Baell, J. B.. (2009) Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with anti-parasitic activity. Antimicrobial agents and chemotherapy : AAC, Vol. 53, H. 7. S. 2824-2833.

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Official URL: http://edoc.unibas.ch/dok/A5843369

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Abstract

A high-throughput screening campaign of 100,000 lead like compounds led to the identification of 9 novel chemical classes of trypanothione reductase (TR) inhibitors worthy of further investigation. Hits from 5 of these chemical classes have been developed further through different combinations of preliminary SAR probing, anti-parasitic, cytotoxicity, and assessment of their chemical and in vitro metabolic properties. This has led to the identification of novel TR inhibitor chemotypes that are drug like and display anti-parasitic activity. For one class a series of analogues have displayed a correlation between TR inhibition and anti-parasitic activity. This paper explores the process of identifying, investigating and evaluating a series of hits from a high-throughput screening campaign.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:American Society for Microbiology
ISSN:0066-4804
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:14 Sep 2012 07:17
Deposited On:14 Sep 2012 06:39

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