Antischistosomal tetrahydro-γ-carboline sulfonamides

Bioorganic & Medicinal Chemistry Letters
2022.0

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 IC<sub>50</sub> values <5 µM against ex vivo Schistosoma mansoni.

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