2021
DOI: 10.1038/s41598-021-02792-0
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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 (E… Show more

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Cited by 17 publications
(17 citation statements)
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“…For in vivo efficacy studies, female mice were each infected subcutaneously with 80 S. mansoni cercariae. Then, animals were randomly divided into experimental groups (five mice per group), and asiaticoside and PZQ were administered at single oral doses (400 mg/kg), by oral gavage, 49 days post infection (adult worm stage, patent infection) [ 1 , 2 , 3 ]. Group I: asiaticoside (400 mg/kg), which was dissolved in 2% ethanol in PBS ( v / v ); group II: control group, which was infected and received treatment only with vehicle (2% ethanol in PBS v / v ); and group III: PZQ (400 mg/kg, p.o.)…”
Section: Methodsmentioning
confidence: 99%
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“…For in vivo efficacy studies, female mice were each infected subcutaneously with 80 S. mansoni cercariae. Then, animals were randomly divided into experimental groups (five mice per group), and asiaticoside and PZQ were administered at single oral doses (400 mg/kg), by oral gavage, 49 days post infection (adult worm stage, patent infection) [ 1 , 2 , 3 ]. Group I: asiaticoside (400 mg/kg), which was dissolved in 2% ethanol in PBS ( v / v ); group II: control group, which was infected and received treatment only with vehicle (2% ethanol in PBS v / v ); and group III: PZQ (400 mg/kg, p.o.)…”
Section: Methodsmentioning
confidence: 99%
“…Schistosomiasis, caused by helminth parasites of the genus Schistosoma , is a neglected tropical disease with an estimated global prevalence of 240 million infected people in 78 countries and significant mortality and social and economic consequences [ 1 , 2 , 3 ]. Praziquantel (PZQ) is the only drug currently available for the treatment of all Schistosoma species [ 2 , 3 , 4 , 5 ], including Schistosoma mansoni , which is the species prevalent in South America, the Middle East, and Africa [ 1 , 3 , 6 ]. However, despite its effectiveness, PZQ has no efficacy against juvenile worms, which is a limit to schistosomiasis control and elimination [ 1 , 4 , 5 ].…”
Section: Introductionmentioning
confidence: 99%
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