Title |
Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice
|
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Published in |
Bioorganic & Medicinal Chemistry, March 2015
|
DOI | 10.1016/j.bmc.2015.02.061 |
Pubmed ID | |
Authors |
Igor M. Opsenica, Tatjana Ž. Verbić, Mikloš Tot, Richard J. Sciotti, Brandon S. Pybus, Olgica Djurković-Djaković, Ksenija Slavić, Bogdan A. Šolaja |
Abstract |
We herein report the design and synthesis of a novel series of thiophene- and furan-based aminoquinoline derivatives which were found to be potent antimalarials and inhibitors of β-hematin polymerization. Tested compounds were 3-71 times more potent in vitro than CQ against chloroquine-resistant (CQR) W2 strain with benzonitrile 30 being as active as mefloquine (MFQ), and almost all synthesized aminoquinolines (22/27) were more potent than MFQ against multidrug-resistant (MDR) strain C235. In vivo experiments revealed that compound 28 showed clearance with recrudescence at 40mg/kg/day, while 5/5 mice survived in Thompson test at 160mg/kg/day. |
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Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 1 | 50% |
United Kingdom | 1 | 50% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 2 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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United Kingdom | 2 | 8% |
United States | 1 | 4% |
Unknown | 21 | 88% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Bachelor | 4 | 17% |
Student > Ph. D. Student | 4 | 17% |
Other | 3 | 13% |
Researcher | 3 | 13% |
Lecturer | 2 | 8% |
Other | 4 | 17% |
Unknown | 4 | 17% |
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Medicine and Dentistry | 5 | 21% |
Chemistry | 4 | 17% |
Biochemistry, Genetics and Molecular Biology | 2 | 8% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 8% |
Immunology and Microbiology | 2 | 8% |
Other | 4 | 17% |
Unknown | 5 | 21% |