Antischistosomal tetrahydro-γ-carboline sulfonamides.
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ABSTRACT: We discovered tetrahydro-γ-carboline sulfonamides as a new antischistosomal chemotype. The aryl sulfonamide and tetrahydro-γ-carboline substructures were required for high antischistosomal activity. Increasing polarity improved solubility and metabolic stability but decreased antischistosomal activity. We identified two compounds with IC50 values <5 µM against ex vivo Schistosoma mansoni.
SUBMITTER: Ren R
PROVIDER: S-EPMC8826590 | biostudies-literature | 2022 Mar
REPOSITORIES: biostudies-literature
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