Discovery and structure-activity relationships of pyrrolone antimalarials

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.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/dok/A6124624

Downloads: Statistics Overview


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)
UniBasel Contributors:Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
Note:Publication type according to Uni Basel Research Database: Journal article
Related URLs:
Identification Number:
Last Modified:05 Dec 2017 10:26
Deposited On:16 Aug 2013 07:31

Repository Staff Only: item control page