| Autor: |
Brian, Cox, James, Duffy, Victor, Zdorichenko, Corentin, Bellanger, Jessica, Hurcum, Benoît, Laleu, Kevin I, Booker-Milburn, Luke D, Elliott, Michael, Robertson-Ralph, Christopher J, Swain, Stephen J, Bishop, Irene, Hallyburton, Mark, Anderson |
| Rok vydání: |
2020 |
| Zdroj: |
ACS Med Chem Lett |
| ISSN: |
1948-5875 |
| Popis: |
[Image: see text] We utilized synthetic photochemistry to generate novel sp(3)-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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