Novel 1<i>H</i>-1,2,3-Triazole Derivatives of Praziquantel with TRPM_PZQ Modulatory Activity and Antiparasitic Effects on Larvae, Juvenile, and Adult Worms of <i>Schistosoma mansoni</i>.

ABSTRACT: The identification of a transient receptor potential ion channel of the melastatin subfamily activated by praziquantel (TRPM_PZQ) has opened new opportunities for target-based schistosomiasis drug discovery. In this study, eight new 1H-1,2,3-triazole derivatives of praziquantel (PZQ), and their synthetic intermediates, were prepared and evaluated for their schistosomicidal activity on schistosomula, juvenile, and adult Schistosoma mansoni. Their ability to activate schistosome wild-type (WT) and mutant TRPM_PZQ (Sm.TRPM_PZQ), as well as a schistosome TRPM channel activated by meclonazepam (Sm.TRPM_MCLZ), and TRPM_PZQ from Fasciola hepatica (Fh.TRPM_PZQ) and Echinococcus granulosus (

SUBMITTER: Junior FPS 

PROVIDER: S-EPMC12718081 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature