Ren, R. and Wang, X. and Leas, D. A. and Häberli, C. and Cal, M. and Dong, Y. and Kaiser, M. and Keiser, J. and Vennerstrom, J. L.. (2022) Antischistosomal tetrahydro-γ-carboline sulfonamides. Bioorganic & medicinal chemistry letters, 59. p. 128546.
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Official URL: https://edoc.unibas.ch/90794/
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Abstract
We discovered tetrahydro- gamma -carboline sulfonamides as a new antischistosomal chemotype. The aryl sulfonamide and tetrahydro- gamma-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 microM against ex vivo Schistosoma mansoni.
| Faculties and Departments: | 09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) 09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Helminth Drug Development (Keiser) 09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser) |
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| UniBasel Contributors: | Häberli, Cécile and Cal, Monica and Kaiser, Marcel and Keiser, Jennifer |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| ISSN: | 0960-894X |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 27 Dec 2022 15:56 |
| Deposited On: | 27 Dec 2022 15:56 |
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