@article{edac55e48c524007882cf4321d1b63ab,
title = "Antischistosomal tetrahydro-γ-carboline sulfonamides",
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.",
keywords = "Antischistosomal, SAR, Sulfonamides, Tetrahydro-γ-carboline",
author = "Rongguo Ren and Xiaofang Wang and Leas, {Derek A.} and C{\'e}cile H{\"a}berli and Monica Cal and Yuxiang Dong and Marcel Kaiser and Jennifer Keiser and Vennerstrom, {Jonathan L.}",
note = "Funding Information: We acknowledge the U.S. National Institutes of Health (2R01AI116723-06) and the Swiss National Science Foundation (No. 320030 175585) for financial support. The Centre for Drug Candidate Optimisation, Monash University, Australia is acknowledged for conducting the physicochemical and in vitro ADME screening assays. Funding Information: We acknowledge the U.S. National Institutes of Health (2R01AI116723-06) and the Swiss National Science Foundation (No. 320030 175585) for financial support. The Centre for Drug Candidate Optimisation, Monash University, Australia is acknowledged for conducting the physicochemical and in vitro ADME screening assays. Publisher Copyright: {\textcopyright} 2022 Elsevier Ltd",
year = "2022",
month = mar,
day = "1",
doi = "10.1016/j.bmcl.2022.128546",
language = "English (US)",
volume = "59",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
}