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Discovery of 2-(1H-imidazo-2-yl)piperazines as a new class of potent and non-cytotoxic inhibitors of Trypanosoma brucei growth in vitro

Ferrigno, Federica and Biancofiore, Ilaria and Malancona, Savina and Ponzi, Simona and Paonessa, Giacomo and Graziani, Rita and Bresciani, Alberto and Gennari, Nadia and Di Marco, Annalise and Kaiser, Marcel and Summa, Vincenzo and Harper, Steven and Ontoria, Jesus M.. (2018) Discovery of 2-(1H-imidazo-2-yl)piperazines as a new class of potent and non-cytotoxic inhibitors of Trypanosoma brucei growth in vitro. Bioorganic & medicinal chemistry letters, 28 (23-24). pp. 3689-3692.

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Official URL: https://edoc.unibas.ch/67909/

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Abstract

The identification of a new series of growth inhibitors of Trypanosoma brucei rhodesiense, causative agent of Human African Trypanosomiasis (HAT), is described. A selection of compounds from our in-house compound collection was screened in vitro against the parasite leading to the identification of compounds with nanomolar inhibition of T. brucei growth. Preliminary SAR on the hit compound led to the identification of compound 34 that shows low nanomolar parasite growth inhibition (T. brucei EC; 50; 5 nM), is not cytotoxic (HeLa CC; 50; > 25,000 nM) and is selective over other parasites, such as Trypanosoma cruzi and Plasmodium falciparum (T. cruzi EC; 50; 8120 nM, P. falciparum EC; 50; 3624 nM).
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:Elsevier
ISSN:0960-894X
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:15 Jan 2019 13:59
Deposited On:15 Jan 2019 13:59

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