Wang, X. and Cal, M. and Kaiser, M. and Buckner, F. S. and Lepesheva, G. I. and Sanford, A. G. and Wallick, A. I. and Davis, P. H. and Vennerstrom, J. L.. (2019) A new chemotype with promise against Trypanosoma cruzi. Bioorganic & medicinal chemistry letters, 30. p. 126778.
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Official URL: https://edoc.unibas.ch/73575/
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Abstract
Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of >/=10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.
| Faculties and Departments: | 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: | Cal, Monica and Kaiser, Marcel |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Pergamon |
| ISSN: | 0960-894X |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 03 Mar 2020 16:00 |
| Deposited On: | 03 Mar 2020 16:00 |
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