Pyrazoline derivatives as promising novel antischistosomal agents.

ABSTRACT: Praziquantel is the only available drug to treat schistosomiasis, a parasitic disease that currently infects more than 240 million people globally. Due to increasing concerns about resistance and inadequate efficacy there is a need for new therapeutics. In this study, a series of 17 pyrazolines (15-31) and three pyrazoles (32-34) were synthesized and evaluated for their antiparasitic properties against ex vivo adult Schistosoma mansoni worms. Of the 20 compounds tested, six had a 50% effective concentration (EC₅₀) below 30 μM. Our best hit, pyrazoline 22, showed promising activity against adult schistosomes, with an EC₅₀ < 10 µM. Additionally, compound 22 had low cytotoxicity, with selectivity index of 21.6 and 32.2 for monkey and human cell lines, respectively. All a

SUBMITTER: Morais CS 

PROVIDER: S-EPMC8648852 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature