| Autor: |
Jakal Amin, Scott Louis Cohen, Brad Snodgrass, Xiao-Hui Chen, Monish Jain, Panos Hatsis, Suzie Ferreira, David Barnes-Seeman, Leslie Bell |
| Rok vydání: |
2013 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 4:514-516 |
| ISSN: |
1948-5875 |
| Popis: |
Susceptibility to metabolism is a common issue with the tert-butyl group on compounds of medicinal interest. We demonstrate an approach of removing all the fully sp(3) C-Hs from a tert-butyl group: replacing some C-Hs with C-Fs and increasing the s-character of the remaining C-Hs. This approach gave a trifluoromethylcyclopropyl group, which increased metabolic stability. Trifluoromethylcyclopropyl-containing analogues had consistently higher metabolic stability in vitro and in vivo compared to their tert-butyl-containing counterparts. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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