Antischistosomal tetrahydro-γ-carboline sulfonamides

Date Issued
2022-01-01
Author(s)
Ren, R.
Wang, X.
Leas, D. A.
Dong, Y.
Vennerstrom, J. L.
DOI
10.1016/j.bmcl.2022.128546
Abstract
We discovered tetrahydro- gamma -carboline sulfonamides as a new antischistosomal chemotype. The aryl sulfonamide and tetrahydro- gamma-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 microM against ex vivo Schistosoma mansoni.