Development of Biarylalkyl Carboxylic Acid Amides with Improved Anti-schistosomal Activity.

ABSTRACT: The parasitic disease schistosomiasis is the cause of more than 200 000 human deaths per year. Although the disease is treatable, there is one major shortcoming: praziquantel has been the only drug used to combat these parasites since 1977. The risk of the emergence of resistant schistosomes is known to be increasing, as a reduced sensitivity of these parasites toward praziquantel has been observed. We developed a new class of substances, which are derived from inhibitors of human aldose reductase, and which showed promising activity against Schistosoma mansoni couples in vitro. Further optimisation of the compounds led to an increase in anti-schistosomal activity with observed phenotypes such as reduced egg production, vitality, and motility as well as tegumental damage and gut dilatation

SUBMITTER: Peter Ventura AM 

PROVIDER: S-EPMC7687077 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature