Zhang, Huaisheng and Collins, Jasmine and Nyamwihura, Rogers and Ware, Shelbi and Kaiser, Marcel and Ogungbe, Ifedayo Victor. (2018) Discovery of a quinoline-based phenyl sulfone derivative as an antitrypanosomal agent. Bioorganic & medicinal chemistry, 28 (9). pp. 1647-1651.
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Official URL: https://edoc.unibas.ch/64895/
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Abstract
A series of natural products-based phenyl sulfone derivative and their property-based analogues were investigated as potential growth inhibitors of Trypanosoma brucei. Trypanosoma brucei is a kinetoplastid protozoan parasite that causes trypanosomiasis. In this work, we found that nopol- and quinoline-based phenyl sulfone derivative were the most active and selective for T. brucei, and they were not reactive towards the active thiol of T. brucei's cysteine protease rhodesain. A thiol reactive variant of the quinoline-based phenyl sulfone was subsequently investigated and found to be a moderate inhibitor of rhodesain. The quinoline-based compound that is not reactive towards rhodesain can serve a template for phenotypic-based lead discovery while its thiol-active congener can serve as template for structure-based investigation of new antitrypanosomal agents.
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) > Parasite Chemotherapy (Mäser) |
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UniBasel Contributors: | Kaiser, Marcel |
Item Type: | Article, refereed |
Article Subtype: | Research Article |
Publisher: | Pergamon |
ISSN: | 0968-0896 |
Note: | Publication type according to Uni Basel Research Database: Journal article |
Identification Number: |
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Last Modified: | 04 Jul 2018 08:57 |
Deposited On: | 04 Jul 2018 08:57 |
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