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.
Original language | English (US) |
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Article number | 128546 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 59 |
DOIs | |
State | Published - Mar 1 2022 |
Keywords
- Antischistosomal
- SAR
- Sulfonamides
- Tetrahydro-γ-carboline
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry