Mizukawa, Y. and Ikegami-Kawai, M. and Horiuchi, M. and Kaiser, M. and Kojima, M. and Sakanoue, S. and Miyagi, S. and Nanga Chick, C. and Togashi, H. and Tsubuki, M. and Ihara, M. and Usuki, T. and Itoh, I.. (2021) Quest for a potent antimalarial drug lead: synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines. Bioorganic & medicinal chemistry, 33. p. 116018.
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Abstract
Quinazolines have long been known to exert varied pharmacologic activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, we have synthesized approximately 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, we summarize the results and report the discovery of 6,7-dimethoxy-N(4)-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine (20, SSJ-717), which exhibits high antimalarial activity as a promising antimalarial drug lead.
| 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 |
| ISSN: | 0968-0896 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Language: | English |
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| Identification Number: |
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| edoc DOI: | |
| Last Modified: | 20 Dec 2022 14:48 |
| Deposited On: | 20 Dec 2022 14:48 |
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