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Activity of diphenyl ether benzyl amines against Human African Trypanosomiasis

Hagen, James P. and Darner, Grant and Anderson, Samuel and Higgins, Katie and Leas, Derek A. and Mitra, Ananya and Mashinson, Victoria and Wol, Tasloach and Vera-Esquivel, Carlos and Belter, Bret and Cal, Monica and Kaiser, Marcel and Wallick, Alexander and Warner, Rosalie C. and Davis, Paul H.. (2020) Activity of diphenyl ether benzyl amines against Human African Trypanosomiasis. Bioorganic chemistry, 97. p. 103590.

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Official URL: https://edoc.unibas.ch/76106/

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Abstract

Insect-borne parasite Trypanosoma brucei plagues humans and other animals, eliciting the disease Human African trypanosomiasis, also known as African sleeping sickness. This disease poses the biggest threat to the people in Sub-Saharan Africa. Given the high toxicity and difficulties with administration of currently available drugs, a novel treatment is needed. Building on known Human African trypanosomiasis structure-activity relationship (SAR), we now describe a number of functionally simple diphenyl ether analogs which give low micromolar activity (IC; 50; = 0.16-0.96 μM) against T. b. rhodesiense. The best compound shows favorable selectivity against the L6 cell line (SI = 750) and even greater selectivity (SI = 1200) against four human cell lines. The data herein provides direction for the ongoing optimization of antitrypanosomal diphenyl ethers.
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:Cal, Monica and Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0045-2068
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:27 Mar 2020 07:02
Deposited On:27 Mar 2020 07:02

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