Laleu, B. and Akao, Y. and Ochida, A. and Duffy, S. and Lucantoni, L. and Shackleford, D. M. and Chen, G. and Katneni, K. and Chiu, F. C. K. and White, K. L. and Chen, X. and Sturm, A. and Dechering, K. J. and Crespo, B. and Sanz, L. M. and Wang, B. and Wittlin, S. and Charman, S. A. and Avery, V. M. and Cho, N. and Kamaura, M.. (2021) Discovery and structure-activity relationships of quinazolinone-2-carboxamide derivatives as novel orally efficacious antimalarials. Journal of medicinal chemistry, 64 (17). pp. 12582-12602.
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Official URL: https://edoc.unibas.ch/89180/
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Abstract
A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide derivatives as a novel antimalarial scaffold. Structure-activity relationship studies led to identification of a potent inhibitor 19f, 95-fold more potent than the original hit compound, active against laboratory-resistant strains of malaria. Profiling of 19f suggested a fast in vitro killing profile. In vivo activity in a murine model of human malaria in a dose-dependent manner constitutes a concomitant benefit.
| 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: | Wittlin, Sergio |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| ISSN: | 0022-2623 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 20 Dec 2022 12:24 |
| Deposited On: | 20 Dec 2022 12:24 |
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