Abstract
The drug praziquantel (PZQ) is an essential medicine for treating schistosomiasis, a parasitic disease that afflicts over 250 million people worldwide. PZQ causes a rapid paralysis of the parasitic blood flukes that cause schistosomiasis, however the flatworm target of PZQ has been undefined since PZQ was discovered in the 1970s. Analysis of the structure-activity relationship (SAR) of a series of >40 PZQ analogues revealed that the SAR for these compounds at causing worm paralysis mirrored the activation of a schistosome transient receptor potential melastatin ion channel (Sm.TRPMPZQ) in vitro.
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