Antischistosomal tetrahydro-γ-carboline sulfonamides. (1st March 2022)

• Record Type: Journal Article
• Authors: Ren, Rongguo; Wang, Xiaofang; Leas, Derek A.; Häberli, Cécile; Cal, Monica; Dong, Yuxiang; Kaiser, Marcel; Keiser, Jennifer; Vennerstrom, Jonathan L.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 59(2022)
• Publication Date: 2022-03-01
• Subjects: Tetrahydro-γ-carboline -- Sulfonamides -- Antischistosomal -- SAR; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2022.128546
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 .