Murugesan, D. and Mital, A. and Kaiser, M. and Shackleford, D. M. and Morizzi, J. and Katneni, K. and Campbell, M. and Hudson, A. and Charman, S. A. and Yeates, C. and Gilbert, I. H.. (2013) Discovery and structure-activity relationships of pyrrolone antimalarials. Journal of medicinal chemistry, 56 (7). pp. 2975-2990.
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Official URL: http://edoc.unibas.ch/dok/A6124624
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Abstract
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC50 approximately 9 nM), good selectivity (<2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalarial
| 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) |
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| UniBasel Contributors: | Kaiser, Marcel |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | American Chemical Society |
| ISSN: | 0022-2623 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Related URLs: | |
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| Last Modified: | 05 Dec 2017 10:26 |
| Deposited On: | 16 Aug 2013 07:31 |
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