| Autor: |
Michael Robertson-Ralph, Mark G. Anderson, Corentin Bellanger, Brian Cox, Benoît Laleu, Luke D. Elliott, James Duffy, Jessica Hurcum, Christopher J. Swain, Victor Zdorichenko, Irene Hallyburton, Kevin I. Booker-Milburn, Stephen J. Bishop |
| Rok vydání: |
2020 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 11:2497-2503 |
| ISSN: |
1948-5875 |
| Popis: |
We utilized synthetic photochemistry to generate novel sp3-rich scaffolds and report the design, synthesis, and biological testing of a diverse series of amides based on the 1-(amino-methyl)-2-benzyl-2-aza-bicyclo[2.1.1]hexane scaffold. Preliminary antimalarial screening of the library provided promising compounds with activity in the 1-5 μM range with an enhanced hit rate. Further evaluation (solubility, drug metabolism and pharmacokinetics (DMPK), and toxicity) of a selected compound (9) suggested that this series represents an excellent opportunity for further optimization with the framework offering multiple opportunities for the addition of uniquely vectorally positioned extra functionality. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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