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Discovery and optimization of a compound series active against Trypanosoma cruzi, the causative agent of chagas disease

Harrison, Justin R. and Sarkar, Sandipan and Hampton, Shahienaz and Riley, Jennifer and Stojanovski, Laste and Sahlberg, Christer and Appelqvist, Pia and Erath, Jessey and Mathan, Vinodhini and Rodriguez, Ana and Kaiser, Marcel and Pacanowska, Dolores Gonzalez and Read, Kevin D. and Johansson, Nils Gunnar and Gilbert, Ian H.. (2020) Discovery and optimization of a compound series active against Trypanosoma cruzi, the causative agent of chagas disease. Journal of medicinal chemistry, 63 (6). pp. 3066-3089.

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Official URL: https://edoc.unibas.ch/76443/

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Abstract

Chagas disease is caused by the protozoan parasite; Trypanosoma cruzi; . It is endemic in South and Central America and recently has been found in other parts of the world, due to migration of chronically infected patients. The current treatment for Chagas disease is not satisfactory, and there is a need for new treatments. In this work, we describe the optimization of a hit compound resulting from the phenotypic screen of a library of compounds against; T. cruzi; . The compound series was optimized to the level where it had satisfactory pharmacokinetics to allow an efficacy study in a mouse model of Chagas disease. We were able to demonstrate efficacy in this model, although further work is required to improve the potency and selectivity of this series.
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 (MPI) > Parasite Chemotherapy (Mäser)
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
Identification Number:
Last Modified:23 Apr 2020 14:47
Deposited On:23 Apr 2020 14:47

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