Antischistosomal tetrahydro-γ-carboline sulfonamides

[Display omitted] 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 antis...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2022-03, Vol.59, p.128546-128546, Article 128546
Hauptverfasser:	Ren, Rongguo, Wang, Xiaofang, Leas, Derek A., Häberli, Cécile, Cal, Monica, Dong, Yuxiang, Kaiser, Marcel, Keiser, Jennifer, Vennerstrom, Jonathan L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antischistosomal Carbolines - chemical synthesis Carbolines - chemistry Carbolines - pharmacology Dose-Response Relationship, Drug Molecular Structure SAR Schistosoma mansoni - drug effects Structure-Activity Relationship Sulfonamides Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacology Tetrahydro-γ-carboline
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Zusammenfassung:	[Display omitted] 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
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2022.128546