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Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility
Introducing a reactive carbonyl to a scaffold that does not otherwise have an electrophilic functionality to create a reversible covalent inhibitor is a potentially useful strategy for enhancing compound potency. However, aldehydes are metabolically unstable, which precludes the use of this strategy...
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| Publicado no: | Bioorg Med Chem Lett |
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| Main Authors: | , , , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
2015
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| Assuntos: | |
| Acesso em linha: | https://ncbi.nlm.nih.gov/pmc/articles/PMC4653046/ https://ncbi.nlm.nih.gov/pubmed/26231156 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.07.018 |
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