Novel lead compounds in pre-clinical development against African sleeping sickness.

Medchemcomm

Institute of Pharmacy and Food Chemistry , University of Würzburg, Am Hubland , 97074 Würzburg , Germany . Email:

Published: October 2017

Human African trypanosomiasis (HAT), also known as African sleeping sickness, is caused by parasitic protozoa of the genus . As the disease progresses, the parasites cross the blood brain barrier and are lethal for the patients if the disease is left untreated. Current therapies suffer from several drawbacks due to toxicity of the respective compounds or resistance to approved antitrypanosomal drugs. In this review, the different strategies of drug development against HAT are considered, namely the target-based approach, the phenotypic high throughput screening and the drug repurposing strategy. The most promising compounds emerging from these approaches entering an evaluation are mentioned herein. Of note, it may turn out to be difficult to confirm activity in an animal model of infection; however, possible reasons for the missing efficacy in unsuccessful studies are discussed.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072528PMC
http://dx.doi.org/10.1039/c7md00280gDOI Listing

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