Antischistosomal tetrahydro-γ-carboline sulfonamides

Rongguo Ren, Xiaofang Wang, Derek A. Leas, Cécile Häberli, Monica Cal, Yuxiang Dong, Marcel Kaiser, Jennifer Keiser, Jonathan L. Vennerstrom

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

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 languageEnglish (US)
Article number128546
JournalBioorganic and Medicinal Chemistry Letters
Volume59
DOIs
StatePublished - 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

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