Abstract
The synthesis and structure-activity relationship (SAR) studies of praziquantel derivatives with activity against adult Schistosoma japonicum are described. Several of them showed better worm killing activity than praziquantel and could serve as leads for further optimization.
Highlights
Schistosomiasis is a neglected tropical disease (NTD) caused by blood-dwelling trematodes belonging to the genus Schistosoma
The racemic PZQ from Aldrich was hydrolyzed by 2 N HCl to yield praziquanamine (1) using the method described by the Vennerstrom group [23], followed by coupling with acyl chlorides to yield compounds 2–12
To extend the structure-activity relationship (SAR) studies, the aromatic moiety was replaced by a thiophene ring, and compound 23 was synthesized using the method described by Frehel and his coworkers [29]
Summary
Schistosomiasis is a neglected tropical disease (NTD) caused by blood-dwelling trematodes belonging to the genus Schistosoma. It has been estimated that some 779 million people are at risk for schistosomiasis transmission, with 207 million infected in 76 countries and territories [1,2]. In China, the disease caused by Schistosoma japonicum remains a major public health concern with more than 280 thousand people infected [3]. PZQ does not prevent reinfection, and it is inactive against juvenile schistosomes. It has only a limited effect on developed liver and spleen lesions, as well as on the emergent schistosome phenotypes that are resistant to PZQ chemotherapy [5,6]
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